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Derivative of diphenyl sulphide, and pharmaceutical product containing it as active ingredient Invention relates to derivative of diphenyl sulphide, that can be used in medicine as antagonist of S1P3 receptor of common formula (1) |
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Method of obtaining aminohydroxydiphosphonic acids Invention relates to a method of obtaining aminohydroxydiphosphonic acids for application in the chemical industry. Claimed is obtaining aminohydroxydiphosphonic acid by the interaction of the respective aminocarboxylic acid and P4O6 at 40°C-180°C in the presence of sulphonic acid. Aminocarboxylic acid and P4O6 are used in molar ratios from 4:1 to 1:1, from 1 to 30 equivalents of sulphonic acid being used per mole of aminocarboxylic acid. Aminocarboxylic acid has formula (A)(B)N-X1-COOH, D-X2-COOH or E-X3-COOH, where X1 and X2 are optionally substituted linear, branched, cyclic or aromatic groups, which have from 2 to 20 carbon atoms; A and B are selected from H or an optionally substituted branched, linear, cyclic, aromatic, heterocyclic or heteroaromatic group, which has from 1 to 20 carbon atoms; D represents an optionally substituted 4-8-membered heteromonocyclic or heteromonoaromatic group, which is bound to X2 via a nitrogen atom, where the substituent can be condensed with D; or D together with X2 represent an imide; X3 represents a bond or an optionally substituted C1-C20 linear, branched, cyclic or aromatic hydrocarbon group, E is an optionally substituted heterocyclic or heteroaromatic 4-14-membered ring, bound to X3 via a carbon atom; heterocyclic and heteroaromatic groups contain from 1 to 4 heteroatoms, selected from N, S and O, the difference between the number of atoms and heteroatoms in the cycles is not less than 2. |
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Method for synthesis of phosphonoalkyliminodiacetic acid Invention relates to the improved method for the manufacture of phosphonoalkyliminodiacetic acid M2PO3-X-N-(CH2COOM)2, wherein X is methylene, M - hydrogen atom, which can be used commercially in chemical industry. The method comprises as follows: the iminodiacetic acid reacts with phosphorous acid and formaldehyde in the presence of phosphoric acid, whereby the molar ratio of phosphorous acid: iminodiacetic acid 1:1, phosphoric acid:phosphorous acid 5:1, formaldehyde:iminodiacetic acid from 1.1:1 to 1:1, at 124-140°C for a period of from 1 minute to 10 hours, to thereby yield a substantially reaction medium insoluble product, separating the insoluble reaction product from the reaction medium, and water washing the insoluble reaction product. |
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Present invention relates to novel compounds of formula T-B for use as dispersants and for inhibiting scaling and a method for production thereof, where B represents -X-N(W)(ZPO3M2), X is a C2-C50 hydrocarbon, optionally substituted with OH or COOH; Z is C1-C6 alkylene; M is H; W is ZPO3M2; T is selected from: (I)MOOC-X-N(U)-; (II) MOOC-C(X2)2-N(U)-; (iii) MOOC-X-S-; (IVi) [X(HO)n(N-U)n]n-; (Vi) U-N(U)-[X-N(U)]n-; (Vii) D-S-; (VIIIi) MOOC-X-O-; (IXi) MOOC-C(X2)2-O; (Xi) NHR"- ; and (XIi) (DCO)2-N-. U is selected from C1-C12 hydrocarbon chains, H and X-N(W)(ZPO3M2); X2 is selected from H, C1-C20 hydrocarbon chains, optionally substituted C1-C12 hydrocarbon groups, which can be substituted with COOH; n', n" and n"' are equal to 1; D and R" are selected from C1-C50 hydrocarbon chains, optionally substituted with COOH; or the compound T-B is 3-phenoxypropylimino-bis-methylenephosphonic acid, wherein the compound T-B is not carboxypropyl-aminopropylimino-N-bis-(methylenephosphonic acid). |
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Method of producing free acids from salts thereof Aqueous ammonium salt solution is reacted with an organic extraction agent selected from a group comprising amines of general formula (0). R1, R2 and R3 are independently identical or different, branched or straight, optionally substituted hydrocarbon residues or a hydrogen atom H, and the salt is split at temperature and pressure at which the aqueous solution and the extraction agent are in liquid aggregate states. An auxiliary medium is added for stripping the carrier gas in order to remove NH3 from the aqueous solution, and a portion of the formed free organic acid is converted to the organic extraction agent. The organic acid is 2-hydroxyisobutyric acid and the extraction agent is dialkylamine. Freed ammonia is removed from the aqueous solution by a continuous gas stream and can be returned to the production process. The free acid can be extracted from the extraction agent using a method such as distillation, rectification, crystallisation, reverse extraction, chromatography, adsorption or by membrane methods. |
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Method of obtaining monoethanolamine salts of phosphonic acids Claimed invention relates to method of obtaining salts of phosphonic acids with improved solubility in highly mineralised waters and water-organic solvents and can be applied in oil and gas industry, heat and power engineering, household chemicals and cleaning, construction, agriculture, food industry. Claimed method includes interaction of phosphonic acid or acidic salt of phosphonic acid with base in water solution, and as base used is monoethanolamine with the following mole ratio of reagents: phosphonic acid or acidic salt of phosphonic acid: monoethanolamine from 1:2 to 1:n, where n is basicity of phosphonic acid, and phosphonic acids are selected from nitrylotrimethylphosphonic acid with n equal 6, diethylenetriaminpentamethylphosphonic acid with n equal 10, 1-hydroxyethane-1,1-diphosphonic acid with n equal 4 and 2-phosphonobutane-1,2,4-carboxylic acid with n equal 5. |
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Crystalline form of a tridecahydrate of tetrasodium nitrilotrismethylene phosphonate zincate relates to a triclinic isometric system, has a spatial symmetry group P 1 ¯ and cell dimensions of the crystal lattice a=1.12208±0.00002 nm, b=1.12666±0.00003 nm, c=1.23286±0.00003 nm, angles between edges of the crystal lattice α=108.455±0.002°, β=97.168±0.002° and γ=117.103±0,002°. The disclosed method includes mixing, in an aqueous solution, nitrilotrimethylene phosphonic acid, zinc oxide and sodium hydroxide in the following ratio, pts.wt: nitrilotrimethylene phosphonic acid - 24…26, zinc oxide - 13…14, sodium hydroxide - 27…30, stirring said mixture while heating, filtering and evaporating the obtained filtrate. |
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Method of producing phthalocyanine mono- and diphosphonic acids Method comprises reacting phthalocyanines with excess phosphorus trichloride or tribromide in the presence of aluminium chloride or bromide, respectively, at temperature of 80-120°C, followed by treatment of the reaction mass with ice, oxidation and further hydrolysis of the separated product. |
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Method of producing aminoalkylene phosphonic acid Invention relates to a method of producing industrially used acids of formula: (X)a[N(W)(Y)2-a]z, where X denotes optionally substituted C1-C200000 linear, branched, cyclic or aromatic hydrocarbon, ZPO3M2, [V-N(K)]n-K, [V-N(Y)]n-V or [V-O]x-V; where V denotes optionally substituted C2-50 linear, branched, cyclic or aromatic hydrocarbon; Y = ZPO3M2, [V-N(K)]n-K or [V-N(K)]n-V; x = 1 to 50000; z = 0 to 200000 and ≤ the number of carbon atoms in X; a = 0 or 1; n = 0 to 50000; Z - C1-6alkylene; M = H; W = H, X and ZPO3M2; K = ZPO3M2 or H. The method includes adding P4O6 to an aqueous reaction medium containing a homogeneous Bronsted acid, wherein P4O6 is hydrolysed to phosphorous acid, and said aqueous medium contains an amine of formula (X)b[N(W)(H)2-b]z, where b = 0 or 1, and the amine is added at the same time as P4O6 or after hydrolysis of P4O6; water after hydrolysis from 0 to 40 wt %, pH during the entire hydrolysis period is kept below 5 with subsequent addition of formaldehyde and a homogenous Bronsted acid with pKa≤3.1 and a heterogeneous Bronsted acid, with the ratios: (a) phosphorous acid, (b) amine, (c) formaldehyde and (d) Bronsted acid: (a):(b) 0.05:1 to 2:1; (c):(b) 0.05:1 to 5:1; (c):(a) 5:1 to 0,25:1; and (b):(d) 40:1 to 1:5; where (a) and (c) denote the number of moles, (b) denotes the number of moles, multiplied by the number of N-H groups in the amine, (d) denotes the number of moles, multiplied by the number of available protons per mole catalyst. |
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Method of obtaining surface-modified mineral material, resulting products and application thereof Invention can be used in the chemical industry. A method of modifying the surface of a mineral material, which is in the form of water sludge or suspension, having pH from 5 to 10, includes addition of, at least, one agent to the said mineral material. The said agent is added in an amount, corresponding to 0.04-1 mg counted per dry weight of the agent per m2 of the total surface of the mineral material. Suspension of the mineral material, which has pH value constituting less than 10 and higher than 7, if a value of an isoelectric point of the said mineral material exceeds 7, and exceeds the value of the isoelecric point of the said material, if the value of the said isoelectric point constitutes 7 or lower. The said agent is in the form of a water solution or a stable water colloid, which has pH lower than 6, and is formed as a result of mixing in a water medium of, at least, one compound, containing phosphonic acid with one or more metal cations or one or more metal-containing cationic compounds. The said metal is selected from the group, consisting of aluminium, zirconium, zinc, cobalt, chrome, iron, copper, tin, titanium and their mixtures. The compound, which contains phosphonic acid and the said cations of metals or the cationic metal-containing compounds, is added in such amount that a molar ratio of phosphonate hydroxyl groups to the metal cation or the metal-containing cationic compound constitutes from 10:1 to 2:1. |
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Phosphorus-containing derivatives of fullerene c60, and their production method Invention refers to fullerenes of formula 1 and to their production methods, which can be used in chemical industry and helioenergetics, , where X means the following: hydrogen atom or alkyl (CnH2n+1; n=1-20) radical, where R1 means the following: hydrogen atom, alkyl (CnH2n+1; n=1-20), alkenyl (CnH2n+1; n=1-20) or alkynyl radical (CnH2n-3; n=1-20); residue of alkyl halide -(CH2)nHal (Hal=F, CI, Br, I), simple ether - (CH2)nOR'1 or -(CH2CH2O)nR'1, for which n=0-20, and R'1 is hydrogen atoms or linear or branched alkyl (CmH2m-1; n=1-20), alkenyl (CmH2m-1; n=1-20) or alkynyl radicals (CmH2m-3, n=1-20). The proposed method consists in the fact that an Arbusov reaction is performed, to which fullerene chloride C60Cl6 is added with the corresponding organic phosphites. |
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Method of producing alkylaminoalkylene phosphonic acids Invention relates to a method of producing alkylaminoalkylene phosphonic acids of formula U-[X-N(W)(ZPO3M2)]S, which can be used in chemical industry. The disclosed method involves reacting a compound of formula Y-X-N(W)(ZPO3M2) with a precursor for groups U, selected from NH3, NH2R', NH(R')2, HOR', NaOH, Na2S, thiourea and Na2S2, where Y is chlorine, X is a C2-C3 linear alkyl, Z is C1 alkylene, M is H; W is ZPO3M2, U is selected from NH2, NHR', N(R')2, NH, N, OH, OR', S, SH and S-S, R' is phenyl or a C1-C3 linear alkyl, s equals 1, if U is NH2, NHR', N(R')2, HS, OR or OH; s equals 2, if U is NH, S or S-S; and s equals 3, if U is N, in an aqueous medium at pH 8 or higher, at temperature from 10°C to 110°C. |
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Invention relates to phosphonate compounds that are suitable as intermediate products when producing dispersants, water treatment agents, scale inhibitors, medicinal agents and detergents, secondary oil recovery agents, fertilisers and micronutrients, having formula: Y-X-N(W) (ZPO3M2), where Y is selected from Cl, I and Br; X is [A-O]x-A, A is a C2-C9 hydrocarbon chain, x equals 1; Z is C1-C3 alkylene; M is selected from H and C1-C6 hydrocarbon chains; W is ZPO3M2; as well as novel methods for production thereof. Said compounds are obtained in an aqueous medium with pH≤6 by reacting a compound of formula halogen--X-NH2, where halogen denotes Cl, Br or I, with phosphorous acid and formaldehyde at 90°-120°C, or by reacting a compound of formula HO-X-N(ZPO3M2)2 at 110°-150°C with an acid selected from hydrochloric acid, hydrobromic acid and hydroiodic acid, under the condition that hydroiodic acid is not used if X contains ether bonds, where X, Z and M assume values given above. |
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Invention relates to protein tyrosine phosphatase 1B inhibitors of the given formula which are suitable for treating diabetes type 2 and cancer, or pharmaceutically acceptable salts thereof, in which X is selected from CH and N; R1 is selected from C1-3alkyl, optionally substituted with 1-3 halogens or one -OH, -CN, -C(=O)H, -C(=O)C1-3alkyl group, -HC=NOH, -(CH3)C=NOH, -HC=NOC1-3alkyl, -(CH3)C=NOC1-3alkyl, -C(=O)OC1-3alkyl, -C(=O)NHR6, -CH=CH-phenyl, in which phenyl is substituted with -C(=O)OH; R3 is a halogen; R6 is selected from H, C1-3alkyl, phenyl, and CH2-phenyl, where phenyl in both cases is optionally substituted with a halogen. |
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Polyalkylene polyamine polymethylphosphonic acid synthesis method Invention relates to a method of producing polyalkylene polyamine polymethylphosphonic acids used as mineral salt deposit inhibitors in heating systems, hot water supply systems and water collection systems of industrial plants. The method involves obtaining polyalkylene polyamine polymethylphosphonic acids, selected from nitrilotrimethylphosphonic acid, methyliminodimethylphosphonic acid, ethylenediamine tetramethylphosphonic acid, hexamethylene diamine tetramethylphosphonic acid, diethylene triamine pentamethylphosphonic acid and triethylene tetraamine hexamethylphosphonic acid, by reacting the corresponding amine or corresponding ammonium compounds with formaldehyde and phosphorous acid in a chloride solution while boiling and then cooling the reaction mass and extracting the end product in solid form, wherein formaldehyde (in form of formalin) is used in 5-7% excess compared to stoichiometry, and the reaction process is carried out at defined conditions for adding starting reagents, where phosphorus acid, hydrochloric acid and formalin are added first, and the corresponding amine or ammonium compound is then added to the formed reaction mixture while stirring for 3-5 minutes. |
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Method of producing biphosphonic acids and their salts Present invention refers to a method of producing biphosphonic acids and their pharmaceutically acceptable salts applied in medicine. In the offered method, the compounds of general formula I or their pharmaceutically acceptable salts where R1 represents alkyl, arylalkyl, an aromatic or heteroaromatic group, are produced by a reaction of carboxylic acid of formula II or its salts, formula II in which R1 has said values, with phosphorous acid and phosphorous trichloride in an aprotonic polar solvent selected from N,N'-dimethylethylene urea (DMEU), N,N'-dimethylpropylene urea (DMPU), 1-methyl-2-pyrrolidone (NMP) or their mixtures. |
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New phosphorus-containing thymomimetic drugs Present invention refers to compounds of formula VIII suitable in medicine as T3 mimetic drugs: VIII, where G is O, -S(=O)2- or -CH2-; R2 is halogen, alkyl, -CF3, -OCF3, alkoxy or cyano; R3 and R4 are H, halogen, alkyl or -(CRa 2)maryl; T is selected from -(CRa 2)k-, -CRb=CRb-(CRa 2)n-, -(CRa 2)n-CRb=CRb, -(CRa 2)-CRb=CRb-(CRa 2)-, O(CRa 2)(CRa 2)n-, -S(CRa 2)(CRa 2)n-, -N(Rc)(CRb 2)(CRa 2)n-, -N(Rb)C(O)(CRa 2)n-, -(CRa 2)nCH(NRbRc) -C(O)(CRa 2)m-, -(CRa 2)mC(O)-, -(CRa 2)C(O)(CRa 2)n-, -(CRa 2)n C(O)(CRa 2)- and -C(O)NH(CRb 2)(CRa 2)p-; Ra, Rb, Rc, R1, R6, R7, R8 and R9 are H, halogen or alkyl; or R6 and T with C atom form a 5-6-members ring with 0-2 groups -NRi-, -O- or -S-; Ri is H, -C(O)alkyl, alkyl or aryl; R5 is OH, alkoxy, -OC(O)Re, -OC(O)ORh, -F, -NHC(O)Re, -NHS(=O)Re, -NHS(=O)2Re, -NHC(S)NH(Rh) or -NHC(O)NH(Rh); Re is alkyl, -(CRa2)n-aryl, -(CRa 2)n-cycloalkyl or -(CRa 2)n- heterocycloalkyl; Rh is H or alkyl; X is P(O)YRllY'Rll; Y and Y' are O or -NRv-; R11 is H, alkyl, -C(Rz)2-OC(O)Ry, -C(RZ)2-O-C(O)ORy, -alkyl-S-C(O)Ry, -[C(Rz)2]q-COORy, -cycloalkylene-COORy, aryl, -C(Rz)2OC(O)SRy, -C(Rx)2COORy or two R11 and R11 form a cycle; k is within 1 to 4; m is within 0 to 3; n is within 0 to 2; p is within 0 to 1; q is 2 or 3; Rv, Rz, Ry and Rx are H or alkyl, or two Rx and Rx form a cycle. |
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Method of producing zoledronic acid Present invention relates to a method of producing zoledronic acid, which is used in treating bone resorption, Paget's disease, hypercalcemia, malignant tumours and metabolic disorders of bone tissue. The disclosed method involves subsequent reaction of 1-(cyanomethyl)imidazole with aqueous solution of methane sulphonic acid at 70-100°C and then with phosphorus trichloride at 50-100°C without extraction of intermediate products in molar ratio 1-(cyanomethyl)imidazole: methane sulphonic acid: phosphorus trichloride equal to 1 : 1.5-3.0 : 1.2-3.0, followed by extraction of the end product using known methods. |
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Invention can be used in medical-cosmetic agents used in case of calcium exchange disorder, which accompanies various diseases. The complexonate is characterised by absorption maximum at 275 nm and can be obtained through incubation in aqueous solution of Na+, K+ of a salt of 1-hydroxyethylidene diphosphonic acid with glucosamine. |
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Method for synthesis of aminopolyalkylene phosphonic acid compounds Aminopolyalkylene phosphonic acid is obtained in the presence of not more than 0.4 wt % halogen of hydrogen acid with respect to phosphorous acid, wherein all N-H groups of the amine are converted to 50% or more of the corresponding alkylene phophonic acids. Reaction of phosphorous acid (a), amine (b) and formaldehyde (c) takes place in the presence of an acid catalyst (d) with pKa ≤ 3.1, which is homogeneous with respect to the reaction medium, in the ratio: (a):(b) between 0.1:1 and 1.5:1, (c):(b) between 0.2:1 and 2:1, (c):(a) between 3:1 and 0.5:1 and (b):(d) between 40:1 and 1:5, where (a) and (c) denote number of moles, (b) denotes number of moles multiplied by number of N-H groups in the amine, (d) denotes number of moles multiplied by number of free protons in one mole of catalyst. |
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Present invention relates to a method of preparing a zinc complex of disodium or dipotassium salt of hydroxyethylidenediphosphonic acid used as a salting and corrosion inhibitor, in agriculture, medicine and biology. The proposed method is realised using raw products in form of hydroxyethylidenediphosphonic acid, zinc oxide and sodium or potassium hydroxide and is distinguished by that, the raw products are mixed simultaneously while adding zinc oxide and sodium or potassium hydroxide to an aqueous solution of hydroxyethylidenephosponic acid in molar ratio equal to 1:2.2-2.6:1.1-1.3, after which the reaction mass is stirred until complete dissolution, cooled, filtering the residue and an aqueous solution of the zinc complex of disodium or dipotassium salt of hydroxyethylidenediphosphonic acid is obtained. |
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Invention relates to a new crystalline polymorph of 3-(N-methyl-N-pentyl)amino-1-hydroxypropane-1,1-diphosphonic acid monosodium salt monohydrate (Ibandronate) with formula I, which is characterised by x-ray powder diffraction pattern with characteristic peaks at angles 2-theta: 9.7°, 12.2°, 14.4°, 16.8° and 25.8°, IR-spectrum with characteristic peaks, cm-1: 3679, 3164, 2955; 2854, 1377, 1290, 1157, 1093, 1068, 1035, 965, 951, 933, 905, 761 and 723, as well as a vibrational Raman spectrum with characteristic peaks, cm-1: 2968, 2951, 2928, 2887, 2849, 1441, 1308, 1136, 1056, 1023, 954, 907, 839, 762 and 678. formula I. |
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Method of producing aminopolyalkylenephosphonic acid compounds in presence of heterogeneous catalyst Disclosed is a method of producing aminoalkylenephosphonic acid which can be used in water purification, inhibiting scum formation, in detergent additives, sequestering agents, activating additives during oil extraction and as pharmaceutical components. The proposed method of producing aminoalkylenephosphonic acid is realised in the presence of not more than 0.4 wt % hydrohalogenic acid, where all available N-H groups in 50% or more of the amine starting material are converted to the corresponding alkylenephosphonic acid. The proposed method involves reacting (a) phosphorous acid, (b) amine and (c) formaldehyde, where the ratio (a): (b) ranges from 0.05:1 to 2:1, (c):(b) ranges from 0.05:1 to 5:1, and (c):(a) ranges from 5:1 to 0.25:1; where (a) and (c) denote number of moles and (b) number of moles multiplied by the number of N-H groups in the amine, in the presence of a Bronsted acid catalyst which is heterogeneous with respect to the reaction medium, with subsequent extraction of the obtained aminoalkylenephosphonic acid. |
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Method of producing mineral salt deposition inhibitor Invention relates to a method of producing mineral salt deposition inhibitors for protecting water circulation systems of enterprises, oilfield equipment and pipelines from mineral deposits, corrosion and biological damage. The method involves reacting ammonia, diethylenetriamine, triethylenetriamine or a technical mixture of polyethylenepolyamines with formaldehyde at temperature ranging from 0 to minus 10°C for two hours, with subsequent reaction with phosphoric acid at 95-96°C, with further neutralisation with sodium hydroxide and addition of methanol and water to the phosphomethylation product, with molar ratio ammonia : formaldehyde : phosphoric acid equal to 1.0 : 2.5-3.0 : 2.5-3.0, diethylenetriamine : formaldehyde : phosphoric acid equal to 1.0 : 5.0 : 5.0, triethylenetriamine : formaldehyde : phosphoric acid equal to 1.0 : 6.0 : 6.0, technical mixture of polyethylenepolyamines : formaldehyde : phosphoric acid equal to 1.0 : 5.0-6.0 : 5.0-6.0. |
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Treatment of m-(phosphomethyl)glycine Material, containing glyphosate, is diluted or suspended in water in the presence of the base with production of composition, including glyphosate salt in water solution of the base then without preliminary concentration and filtration the produced composition is added into acid and precipitated neutralised glyphosate is separated. |
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Polymorphic modification of a ibandronate Invention relates to a new crystalline polymorphic modification of a monohydrate of mon-sodium salt of 3-(N-methyl-N-pentyl)amino-1-hydroxypropane-1,1-diphosphonic acid (ibandronate) of formula 1, used for controlling hypercalcemia. formula 1. |
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Method of obtaining alkali metal salts of n-phosphonomethylglycine Claimed invention relates to method of obtaining alkali metal salts of N-phosphomethylglycine and can be applied in agriculture, for fight against weeds. Claimed method lies in the following: reaction of glyphosate and alkaline reagent interaction is carried out in solid phase in highly efficient mixer in conditions of crashing and in close contact of reaction components. |
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Invention relates to obtaining etyheleneammonium bis(1-hydroxyethane-1,1-diphosphonato(2-))cuprate (+2), etyheleneammonium bis(1-hydroxyethane-1,1-diphosphonato(2-)) zincate(+2) and etyheleneammonium bis(1-hydroxyethane-1,1-diphosphonato(2-)) nickelate(+2) and can be used for processing toxic wastes of obtaining metal coatings - waste electrolytes of galvanic copper, zinc and nickel plating, waste solutions of chemical nickel plating and copper plating. Products, obtained by said method, can be used for preparation of electrolytes, metal corrosion inhibitors, for obtaining various copper, zinc and nickel compounds, including catalysts of organic and inorganic substance synthesis. Claimed method includes using liquid industrial wastes, containing metal(+2), ethyleneammonium and/or anion of 1-hydroxyethane-1,1-diphosphonic acid as reagents. Target products are obtained by crystallisation from reaction water solution with separation of sediment from solution, process is carried out at temperature from (-5) to 105°C and atmospheric pressure. Method allows to obtain pure crystalline products with yield up to 98%, to reduce expenditures on environment protection. |
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Invention relates to novel compounds of formula (I), including its pharmaceutically acceptable salts, solvates, ethers and amides, possessing ability to bind ERα- and ERβ-estrogen receptors, to pharmaceutical composition based on them, to versions of applying claimed compounds in medication preparation and to method of binding ERα- and ERβ-estrogen receptors. (I), where R1 represents H, OH or C1-12alkoxy, or halogen; R2 represents H, OH or halogen; R3 represents C1-12alkyl, halogeno-C1-12alkyl, C3-10cycloalkyl, C1-12alkoxy or C1-12alkoxyC1-12alkyl; R4 represents H or C1-12alkoxy; R5 represents H, halogen or halogeno-C1-12alkyl; R6 represents -(Y)z-R7; R8 represents phenyl or 5- or 6-member heteroaryl, containing N, O or S as heteroatom, where said phenyl and heteroaryl are possibly substituted with OH, halogeno, halogenoC1-12alkyl or C1-12alkoxy. Values R7, Y and z are presented in invention formula. |
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Invention relates to novel chemical compounds as salt-deposition inhibitors and can be used in oil industry in oil extraction, in particular in system of sewage water utilising, as well as in systems of circulating water supply of industrial enterprises. Suggested is complexonate of nitrylotri(methylenephosphonato)-2-phenyl-3-ethyl-8-oxychinolin sodium salt of formula as salt-deposition inhibitor. |
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Long-chain alkylphosphonic acids as soft steel corrosion inhibitors and their production Invention relates to phosphoroorganic chemistry, namely, to method of obtaining long-chain alkylphosphonic acids, possessing anticorrosion activity, based on α-olefins of industrial fraction C16-C18 and C20-C26. Invention can be applied for protection of pipelines, reservoirs, construction metallic structures, equipment for extraction, transportation and processing oil and gas, in metal processing. Long-chain alkylphosphonic acids are obtained by interaction of α-olefins of industrial fraction C16-C18 and C20-C26 with O,O-dimethylphosphorous acid in molar ratio 1:(1.0-2.0) in presence of benzoyl peroxide in amount of 1.0-5.0% of weight of dimethylphosphorous acid at 110-150°C during 10-12 hours in absence of solvent with further hydrolysis of intermediate higher O,O-dimethyl(alkyl) phosphonates with hydrochloric acid with heating, obtaining target product which represents mixture of long-chain alkylphosphonic acids. |
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Invention refers to method of production of amorphous alendronate monosodium and to solid pharmaceutical composition having property to invoke bone bulk expansion and containing therapeutically effective amount of amorphous alendronate monosodium, produced by stated method. Method of production of amorphous alendronate monosodium includes solvent removal from alendronate monosodium solution using spray drying. |
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Acidic phosphorous containing complex forming reagent and method of obtaining it (versions) The invention pertains to an acidic phosphorous containing reagent, is used in the oil industry, heat energy, textile industry, production of mineral fertilizers and household chemistry, and to methods of obtaining the reagent. The reagent (conventional name "АФК-1") contains the following in given mass %: acetoxyethylidenediphosphonic acid 50.0-95.0 mass %, acetic acid - 29.5-0.5 mass %, the rest is acetic anhydride to 100. The quantitative composition of the indicated reagent is determined by the method of obtaining it and the ratios of the initial reagents. The method of obtaining the reagent involves adding acetic anhydride to a suspension of acetic and phosphorous acid at temperature of 60-90°C for a period of 1.5 hours. The reaction mixture is kept at 100-110°C for 1 hour and acidic impurities are distilled off to a controlled volume of distillate. Similar methods are developed based on phosphorous containing wastes from production of acid chlorides of higher fatty acids. The wastes are treated with water or a water solution of acetic acid with subsequent separation of the organic layer of fatty acids, after which the residue, containing phosphorous acid, is treated with phosphorous tri-chloride and acetic anhydride at 115-130°C, and acidic impurities are distilled off to the controlled distillate volume. |
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Acidic phosphorous containing complex-forming reagent and method of obtaining it Invention pertains to the chemistry of phosphorous organic compounds, and specifically to an acidic phosphorous containing complex-forming reagent, which can be used in the oil industry, heat energy, textile industry, production of mineral fertilizers and household chemistry, and to the method of obtaining it. The acidic phosphorous containing complex-forming reagent (conventional name "АФК-2") contains the following in mass %: acetoxyethylidenediphosphonic acid - 50-95 mass %, acetic acid - 50-5 mass %. The method of obtaining the composition involves adding phosphorous tri-chloride, acetic acid and water simultaneously to glacial acetic acid in molar ratios equal to 1:(4.5-5.5):(1.93-1.95), at temperature of 35-45°C with subsequent keeping of the reaction mixture at 110-120°C for a period of 2 hours and controlled distillation of acidic impurities to the required distillate volume. |
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Method of obtaining inhibitor of precipitation of mineral salts Invention pertains to the method of obtaining an inhibitor of precipitation of mineral salts, The inhibitor is obtained by reaction of hexamethylenediamine and ammonium chloride with formaldehyde and phosphorous acid in a medium of diluted hydrochloric acid at high temperature with subsequent neutralisation of the obtained solution using sodium hydroxide to pH of 6.5±1.0. The process is carried out with molar ratio of hexamethylenediamine to ammonium chloride of 1:3-6. |
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Plasma carboxypeptidase b inhibitors Invention describes compound of the formula (I): wherein R1 means hydrogen atom (H); R2 means -SH, -S-C(O)-R8, -P(O)(OR5)2, -P(O)(OR5)R6, -P(O)(OR5)-R7-C(O)-R8, -P(O)(OR5)-R7-N(R5)-S(O)2-R9 or -P(O)(OR5)-R7-N(R5)-C(S)-N(R6)2; R3 means tetrazole, -C(O)OR6, -C(O)O-R7-OC(O)R5; R4 means optionally substituted aryl, or R4 means N-heterocyclyl. Also, invention describes compounds of the formula (II): and (III): wherein X means -CH2- or -O-, and pharmaceutical compositions comprising indicated compounds. Proposed compounds possess inhibitory effect on activity of plasma carboxypeptidase B and used as anti-thrombosis agents. |
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Invention describes a method for synthesis of monohydroperfluoroalkanes, bis-(perfluoroalkyl)phosphinates and perfluoroalkylphosphonates. Method involves treatment of at least one perfluoroalkylphosphorane with at least one base wherein base(s) are chosen from group consisting of alkali-earth metal hydroxides, metalloorganic compound in useful solvent or at least one organic base and an acid in useful reaction medium. Also, invention describes novel perfluoroalkylphosphonates and bis-(perfluoroalkyl)phosphinates, using novel perfluoroalkylphosphonates and bis-(perfluoroalyl)phosphinates as ionic liquids, catalysts of phase transfer or surfactants. |
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Invention relates to a method for preparing copper (II), zinc (II), nickel (II) and cobalt (II) nitrilotri-(methylenephosphonates)(2-) that involves crystallization from aqueous solutions prepared by interaction of metal (II) compound with nitrilotri-(methylenephosphonic) acid or its salt with sodium potassium or ammonium in aqueous medium at temperature from -5°C to 105°C under atmosphere pressure. As a reactive of the metal (II) compound source the waste from manufacturing printing plates and galvanic covers can be used. The end products can be used in preparing the complex electrolytes and solutions for applying metallic covers by electrochemical and chemical methods in aims for inhibition against the equipment corrosion, and for preparing other compounds of metals with nitrilotri-(methylenephosphonic) acid. |
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Phosphonic acid compounds as serine proteinase inhibitors Invention relates to phosphonic acid compounds used as inhibitors of serine proteinase of the general formula (I): wherein R1 is chosen from group comprising piperidinyl, pyrrolidinyl and 1,3,8-triazaspiro[4,5]dec-8-yl (wherein heterocyclic ring as added to nitrogen atom in ring) and -N(R7R80 wherein this heterocyclic ring is substituted optionally with one or two substitutes chosen independently from group comprising the following compounds: (a) C1-C8)-alkyl substituted optionally at terminal carbon atom with a substitute chosen from group comprising aryl, heteroaryl; c) phenyl and naphthalenyl; i) benzothiazolyl; R7 is chosen from group comprising hydrogen atom and (C1-C8)-alkyl; R8 is chosen from group comprising: (aa) (C1-C8)-alkyl; (ab) cycloalkyl; (ac) cycloalkenyl, and (ad) heterocyclyl (wherein R8 is added to carbon atom in ring) wherein (ab) cycloalkyl; (ac) cycloalkenyl, and (ad) heterocyclyl (wherein heterocyclyl (ad) comprises at least one cyclic nitrogen atom) substitutes and cycloalkyl moiety (aa) of a substitute is substituted optionally with substitutes chosen independently from group comprising: (ba) (C1-C8)-alkyl substituted at terminal carbon atom with a substitute chosen from group comprising amino-group (with two substitutes chosen independently from group comprising hydrogen atom and (C1-C8)-alkyl); (bb) (C1-C8)-alkoxy-group substituted at terminal carbon atom with a substitute chosen from group comprising carboxyl; (bc) carbonyl substituted with a substitute chosen from group comprising (C1-C8)-alkyl, aryl, aryl-(C2-C8)-alkenyl; (bd) aryl; (be) heteroaryl; (bf) amino-group substituted with two substitutes chosen independently from group comprising hydrogen atom and (C1-C8)-alkyl; (bh) halogen atom; (bi) hydroxy-group; (bk) heterocyclyl wherein (bd) is aryl substitute, and heteroaryl moiety (bc) comprise a substitute (halogen atom)1-3; R4 is chosen from group comprising aryl and heteroaryl wherein heteroaryl comprises halogen atom as a substitute; R2 and R3 are bound with benzene ring and represent hydrogen atom, and R2 and R3 form in common optionally at least one ring condensed with benzene ring forming polycyclic system wherein this polycyclic system is chosen from group comprising (C9-C14)-benzocondensed cycloalkenyl, (C9-C14)-benzocondensed phenyl; R5 is chosen from group comprising hydrogen atom and (C1-C8)-alkyl; R6 is chosen from group comprising (C1-C8)-alkyl and hydroxy-group; Y is absent, and X represents a single substitute that is added by a double bond and represents oxygen atom (O), and Z is chosen from group comprising a bond, hydrogen atom, and its salts. Also, invention relates to a method for synthesis of these compounds, to their composition inhibiting serine proteinase and to a method for its preparing. Proposed invention describes a method for treatment of inflammatory or serine proteinase-mediated disorder. |
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Method for preparing n-phosphonomethylglycine Invention relates to a novel method for synthesis of N-phosphonomethylglycine. Method involves interaction of hexahydrotriazine compound with triacyl phosphite in organic solvent, saponification of formed phosphonic compound after preliminary extraction into aqueous phase, separation of organic phase and precipitation of N-phosphonomethylglycine by pH value control in the range from 0.5 to 2.0. Invention prevents decomposition of an organic solvent in saponification. |
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The invention is pertaining to the method of production of the water solutions of disodium or dipotassium salt of zinc oxyethyledene phosohonate with concentration of 15-23 % used as the mineral salts sediments inhibitors and as the microfertilizers and having the properties to inhibit corrosion. The method provides for interaction of the water solution of the sodium zincate or the potassium zincate with the 20-60 % water solution of the oxyethyledenephosphonic acid at the temperature of 60-80°С. As a rule, the sodium zincate or the potassium zincate are produced by interaction of 5-20 % water solution of the sodium hydroxide or the potassium hydroxide with zinc oxide at the temperature of 50-75°С at the molar relation of 2:1. |
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Composition contains 10-25% sodium alkylaminophosphonates having general formula: , in which n=9-19, 1-5% sodium chloride, and 70-89% water. Composition is prepared by heat treatment of industrial-grade aliphatic amines with phosphorous acid and formaldehyde. In particular, treatment of aliphatic amines of formula CH3-(CH2)-NH2 (n=9-19) is carried out in presence of hydrochloric acid as catalyst at 95-105°C for 1.5-3.0 h followed by cooling and neutralization with sodium alkali to pH 10. |
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Method for preparing crystalline nitrilotrimethylphosphonic acid disodium salt monohydrate Invention relates to technology for synthesis of crystalline nitrilotrimethylphosphonic acid sodium salts. For synthesis of nitrilotrimethylphosphonic acid disodium salt monohydrate the method involves preliminary synthesis of nitrilotrimethylphosphonic acid by interaction of phosphorus trichloride, formaldehyde and ammonia or its derivative followed by neutralization with sodium hydroxide in the content in the reaction mass 46-54 wt.-% of nitrilotrimethylphosphonic acid and 6.0-16.0 wt.-% of hydrogen chloride up to pH value 2.5-4.5, and isolation of the end compound by crystallization. The mass part of the main substance in synthesized product is 88-95%, the content of chloride ions is 1.2-2.0%, yield is 50-60% as measured for PCl3. Synthesized compound is recommended for using as chelate compounds as a component of detergents, anti-rheological additive in drilling solutions, plasticizing agents for building concretes, in wine-making industry, as inhibitors of salt depositions in heat and power engineering and others fields. |
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Method for preparing bis-(1-hydroxyethane-1,1-diphosphonate(1-)) zinc (ii) Invention relates to the improved method for preparing bis-(1-hydroxyethane-1,1-diphosphonate(1-)) zinc (II). Method involves interaction of zinc-containing reagent and 1-hydroxyethane-1,1-diphosphonic acid in a solvent medium, crystallization of the end product from solution, separation of deposit from solution and drying the deposit. Method involves using water-soluble zinc (II) salt with anion of strong acid as a zinc-containing reagent and preparing the solution with the concentration of zinc (II) salt from 0.2 to 2.2 mole/l and the concentration of 1-hydroxyethane-1,1-diphosphonic acid from 0.4 to 5.0 mole/l. The end product prepared by proposed method can be used in preparing phosphonate electrolytes for galvanic zinc-plating, for preparing zinc-phosphate inhibitors of steel corrosion, as trace supplement to vitamin preparations and fodders for animals, as a zinc microfertilizer in agriculture and for preparing other compounds of zinc (II). Invention provides enhancing purity and uniformity of the end product, increasing its yield, improved technological effectiveness of process, utilizing toxic waste in galvanic manufacturing. |
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Stimulator of growth agricultural root crop plants Invention describes bis-(diethylammonium)-dihydrogen-1-hydroxyethyl-1,1diphosphonate monohydrate of the formula (I) showing properties of stimulator of growth o agricultural root crop plants. Invention provides enhancing productivity of root crops beet and carrot and expanding assortment of agents for this designation. |
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Method for preparing copper (ii) bis-(1-hydroxyethane-1,1-diphosphonate (1-)) from production waste Invention relates to technology of organic substances, in particular, to the improved method for preparing copper (II) bis-(1-hydroxyethane-1,1-diphosphonate (1-)). The final copper (II) bis-(1-hydroxyethane-1,1-diphosphonate (1-)) is prepared by crystallization from aqueous solution with concentrations of copper salt (II) from 0.5 to 2.0 mole/l and 1-hydroxyethane-1,1-diphosphonic acid with concentration from 2.0 to 6.0 mole/l prepared by using copper-containing waste in galvanic and electronic engineering manufacture, or by using a semi-finished product from production of 1-hydroxyethane-1,1-diphosphonic acid. Invention provides reducing cost in production of copper (I) bis-(1-hydroxyethane-1,1-diphosphonate (1-)) in combination with retaining purity, expanded raw base for preparing the end product and utilization of manufacture waste. |
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Method for preparing n-phosphonomethylglycine Invention relates to a method for preparing N-phosphonomethylglycine. Invention describes a method for preparing N-phosphonomethylglycine from an aqueous mixture containing dissolved N-phosphonomethylglycine, ammonium halides, alkali or earth-alkali metal halides and, optionally, organic impurities. Method involves (a) using a mixture with pH value from 2 to 8; (b) separation of mixture is carried out on a selective nanofiltration membrane, and retentate enriched with N-phosphonomethylglycine and depleted with halides and permeate depleted with N-phosphonomethylglycine are obtained, and (c) N-phosphonomethylglycine is isolated from retentate. Method provides preparing N-phosphonomethylglycine in simultaneous separation of halide salts. |
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Method for preparing nickel (ii) bis-(1-hydroxyethane-1,1-diphosphonate (1-)) Method involves preparing nickel (II) bis-(1-hydroxyethane-1,1-diphosphonate (1-)) by addition 1-hydroxyethane-1,1-diphosphonic acid in the concentration 0.2-4.5 mole/l to an aqueous solution containing nickel (II) in the concentration 0.1-2.0 mole/l and organic solvent mixing with water followed by crystallization of the end substance from the solution. Method provides preparing the pure homogeneous end product with high yield, and utilization of depleted electrolyte in nickel plating representing a toxic waste in galvanic manufacture. |
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New acyclic nucleoside phosphonate derivatives, their salts and method for preparing these compounds Invention relates to acyclic nucleoside phosphonate derivatives of the formula (1): wherein means a simple or double bond; R1 means hydrogen atom; R2 and R3 mean hydrogen atom or (C1-C7)-alkyl; R7 and R8 mean hydrogen atom or (C1-C4)-alkyl; R4 and R5 mean hydrogen atom or (C1-C4)-alkyl possibly substituted with one or more halogen atoms, or -(CH2)m-OC(=O)-R6 wherein m means a whole number from 1 to 5; R6 means (C1-C7)-alkyl or 3-6-membered heterocycle comprising 1 or 2 heteroatoms taken among the group consisting of nitrogen (N) and oxygen (O) atoms; Y means -O-, -CH(Z)-, =C(Z)-, -N(Z)- wherein Z means hydrogen atom, hydroxy-group or halogen atom, or (C1-C7)-alkyl; Q (see the claim invention); its pharmaceutically acceptable salts or stereoisomers. Also, invention proposes methods for preparing compounds of the formula (1) and their using in treatment of hepatitis B or preparing a medicinal agent designated for this aim. |
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Chloride removing in method for preparing phosphonomethyliminodiacetic acid Invention relates to a selective method for removing chloride as NaCl from waste in method for preparing N-phosphonomethyliminodiacetic acid. The waste flow is neutralized with NaOH to pH value about 7, water is evaporated from flow of neutralized waste under atmospheric or lower pressure at temperature from 40°C to 130°C until to precipitation of NaCl. The precipitate is filtered off at temperature from 35°C to 110°C to isolate NaCl from filtrate and NaCl is washed out with saturated saline solution. Invention provides effective removal of NaCl from waste in a method for manufacturing N-phoaphonomethyliminodiacetic acid. |
Another patent 2551271.