The method of obtaining imidazo-pyridines or their acid additive salts, imidazo-pyridine.

 

(57) Abstract:

Usage: as compounds with activity improves cognitive activity. The inventive product-imidazopyridine f-ly I with certain values radicals. Getting lead by reaction of the compound f-crystals II with compound f-ly III and the release of free base or acid salt additive. 2 S. and 2 C. p. F.-ly. The structure of the compounds f-l I, II, III:

< / BR>
< / BR>

The invention concerns imidazolylalkyl-pyridines, their production, their use as pharmaceutical agents, and pharmaceutical preparations containing them.

Provides compounds of formula I

< / BR>
(I) in which R1is alkyl (1-4 C), halogen with an atomic number of from 9 to 35, or amino, possibly mono - or disubstituted by alkyl (1-4 C).

R2and R3independently from each other are hydrogen or alkyl (1-4 C), and

R4is hydrogen, hydroxy-alkyl (1-4 C) alkoxy (1-4 C) or halogen with an atomic number of from 9 to 35, in free base form or attached salts of acids which are further referred to as new connections.

Concerning the mentioned alkyl or alkoxy is carbon, in particular, denote methyl or methoxy.

Imidazolylalkyl radical in the preferred embodiment, is located at position 2 of the pyridine.

R1is preferred variant of the stands.

R2and R3in the preferred embodiment, are each hydrogen,

R4is in a preferred embodiment, hydrogen. The compound of example 1 is preferred.

In a special group of new compounds R1is alkyl (1-4 C), R2and R3independently from each other are hydrogen or alkyl (1-4 C), and R4is hydrogen, alkyl (1-4 C) or halogen with an atomic number of from 9 to 35.

In accordance with the invention the new compounds produced as a result of interaction of the compounds of formula II

< / BR>
(II) in which R4have been defined above and X is halogen, with a compound of formula III

< / BR>
(III) in which R1, R2and R3you have already identified, and retrieve the resulting compounds of formula (I) in free base form or in the form annexed acid salt.

The reaction of the compound of formula (II) with the compound of the formula (III) can be performed using known techniques is Shem alcohol. In the formula (II) X is in the preferred embodiment, the chlorine.

Processing the thus obtained reaction mixtures and purification of the compounds of formula (I) can be carried out in accordance with known techniques.

The compounds of formula (I) may be in free form or in the form attached salts of acids. Attached salts of the acids can be obtained from the free bases by means of known techniques and Vice versa.

The initial compounds of formulas (II) and (III) are known or can be obtained in accordance with known techniques, or by analogy with known methods.

The compounds of formula (I) and their acceptable from a pharmaceutical standpoint, salt, hereinafter referred to as compounds that are the subject of the invention show interesting pharmacological activity and can be used so as pharmacological agents.

In the cycle of sleep-wakefulness in rats with inserted into the long tube (according to the method described by J.-M. Vigouret and other J. Pharmacol, T. 10, 503 S. (1978)) compounds, which are the subject of the invention, applied at a dose of 1-100 mg/kg by mouth, lead to an increase in time awake. In addition, p is to be placed, subject of the invention significantly improves the efficiency of recognition, which is measured by the ability to avoid electric shock in a closed box.

A procedure similar to that described V. Haroutunian, etc. in Brain Research, T. 507, 1990, S. 261-266. Male OFA rats (weighing 300 g) were subjected to anesthesia pentobarbital and placed in a stereotaxic installation with the top edge of the cutter set at 5 mm (LC) or 3.3 mm (NBM) below miasnoi line. Unpleasant signals were applied using generator "bad" frequencies at a temperature of 60aboutC for 10 seconds After five weeks after this treatment was carried out by the test behavior test on active avoidance in a closed box, as described in A. R. Rravid, A.-L. Jaton and E. B. Van Deuson in Experimental Brain, Res. Suppl. 13, S. 249, 1986.

Compounds that are the subject of the invention, useful in the treatment of senile dementia, diseases Alzheimer and other degenerative diseases, such as Huntington's chorea, a complex of Parkinson's syndrome Steele-Richardson, late dyskinesia, hyperkinesia, acute confusion, down's syndrome, myasthenia gravis and Friedrich's ataxia, as well as antidepressants.

The daily dose varies in the region from the example of individual doses up to four times per day.

Compounds that are the subject of the invention may be applied by any known method, in particular through the small intestine, in the preferred embodiment, tematicheskim way, for example in the form of tablets, capsules, or parenterally, for example in the form injectively solutions or suspensions.

As indicated in accordance with the invention, a compound for use as a pharmaceutical agent, for example, for the treatment of senile dementia, diseases Alzeimer and other degenerative diseases, such as Huntington's chorea, a complex of Parkinson's syndrome Steele-Richardson, late dyskinesia, hyperkinesia, acute confusion, down's syndrome, myasthenia gravis and Friedrich's ataxia, as well as for the treatment of depression States.

In addition, in accordance with the invention features a pharmaceutical composition comprising a compound which is the subject of the invention, together with at least one pharmaceutical carrier or diluent. Such compositions can be obtained in a known manner. Form of unit doses contain, for example, from about 0.25 mg to about 50 mg of the compounds that are the subject of the invention.

9.3 g of the obtained base in ethanol was mixed with 12.7 g of fumaric acid. The resulting bis(base) Tris(hydrogen fumarate) was led from ethanol ethyl acetate, and then subjected to recrystallization once from ethanol-ethyl acetate. He was confirmed using thin layer chromatography and he melted at a temperature 109-110aboutC.

Following [2-(imidazol-1-yl)methyl] pyridine and [4-(imidazol-1-yl) methyl] pyridine (example 5) was obtained using a procedure similar to the one used in example 1. The results are shown in the table.

1. The method of obtaining imidazo-pyridines of the formula I

< / BR>
where R1WITH1WITH4-alkyl,

in the form of free bases or acid additive salts, characterized in that interact the compounds of formula II

< / BR>
where is m the compounds obtained in free base form or acid additive salt.

2. Imidazo-pyridine formula

< / BR>
where R1WITH1WITH4-alkyl,

in the form of free bases or acid additive salts.

3. Connection on p. 2 representing [2-(2-methylimidazo-1-yl)methyl]pyridine in the form of a free base or an acid additive salt.

4. Connection PP.2 and 3, with activity improves cognitive activity.

 

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The invention relates to new biologically active compounds derived pyrimidine-4-or their pharmaceutically acceptable salts with serotoninergicheskoi, dopaminergically, antihistaminic activity, and compositions on their basis

The invention relates to new biologically active chemical compounds, namely, to derive a cyclic amide of the formula I

R1-(CH2)n-Z,

where R1group cyclic amide, such as 2H-3,4-dihydro-1,3-benzoxazin-2-she, 2H-3,4-dihydro-1,3-benzoxazin-2,4-dione, and 1,2,3,4-tetrahydroquinazoline-2,4-dione, and 1,2,3,4-tetrahydroquinazolin-2-it, 1,2,3,4-tetrahydropyrido(3,2-d)-pyrimidine-2,4 - dione, and 1,2,3,4-tetrahydropyrido(3,2-d)pyrimidine-2-it, 1,2,3,4-tetrahydropyrimidine-2,4-dione, pyrrolidin-2-it, 1,2,3,4 - tetrahydropyridine-2-it, 5H-6,7,8,9-tetrahydropyrido(3,2-b)azepin-6-she N-5,6,7,8-tetrahydropyrido(2,3-b)azepin - 8-she, 2H-3,4-dihydropyrido(2,3-e)-1, 3-oxazin-2-thione or 2-she pyrrolidine (3,4-b)-pyrazin-5-she 1H-2,3,4,5-tetrahydrothieno(2,3-b)indol-2-it, 8H-4,5,6,7-tetrahydrothieno(2,3-b)thiophene-7-she 4H-pyrazolo(5,4-f)benzazepin-9-it, isoindoline-1,3-dione, benzoxazolyl-2-it, unsubstituted or substituted lower alkyl, lower alkoxy, halogen, the nitro-group, carboxy, benzoyl or benzyl, n is zero or an integer from 1 to 6, Z is a group of formula (A) or (B):

N-(CH2)mR2(A) or -(CH2)p, dioxolane, furan, tetrahydrofuran, methylfuran or thiophene, m is an integer from 1 to 3; R3is lower alkyl; R4is phenyl or a radical of dioxolane, furan or thiophene, p = 1, provided that when R1radical 1,2,3,4-tetrahydrobenzo-2-or 1,2,3,4-tetrahydroquinazoline-2,4-dione, R2and R4are not phenyl or substituted by a halogen phenyl, or their pharmacologically acceptable salts with antiacetylcholinesterase activity

The invention relates to new imidazole derivative of General formula I

where R1-COOH or the group< / BR>
R2=H-C3H7or n-C4H9;

R3-Cl, CF3C2F5C6H5or COOH;

R4-COOH, CHO, or CH2HE, provided that

a) when R4-CH2OH, R3-C2F5and R2-n-C3H7,

b) when R3-COOH, R4also is COOH,

b) when R2-n-C3H7, R3-C2F5and R4-COOH, R1is the groupwhich inhibit the action of the hormone angiotensin and can be used in medicine

FIELD: organic chemistry, chemical technology, insecticides.

SUBSTANCE: invention describes new compounds of the formula (X): wherein R1 means -CH2-Het; R means unsubstituted (C1-C20)-alkyl or (C1-C20)-alkyl that is substituted with one or some phenyls, or it means unsubstituted phenyl or phenyl substituted with (C1-C6)-alkyl, or it means (C1-C6)-alkyl that is substituted with cyclohexyl or means unsubstituted (C3-C7)- cyclohexyl or substituted with one or some substitutes taken among the group including halogen atom and (C1-C6)-alkyl, or it means biphenyl, or phenoxyphenyl; T and U each means independently from one another (C1-C6)-alkyl; R2, R'2 mean hydrogen atom; Het means pyridyl that is substituted with halogen atom. Also, invention describes a method for preparing compound of the formula (X) by interaction of compound of the formula (XX) with acid R-COOH and isolation of the end product from reaction mixture wherein substitutes R, R1, R2, R'2, T and U have values indicated for the formula (X); Hal means halogen atom. Also, invention describes a parasiticidal composition for control of blood-sucking insects. Invention provides preparing compounds eliciting parasiticidal activity with expressed prolonged effect.

EFFECT: improved preparing method, valuable properties of compounds and composition.

11 cl, 8 tbl, 8 ex

FIELD: organic chemistry, medicine, pharmacology.

SUBSTANCE: invention relates to new derivatives of carbamic acid esters of the general formula (I):

and their pharmaceutically acceptable salts eliciting activity with respect to metabotropic glutamate receptors mGlu of group I that can be used for treatment of acute and/or chronic neurological disorders. In the general formula (I) R1 means hydrogen atom or (C1-C7)-alkyl; R2 and R2' mean independently of one another hydrogen atom, (C1-C7)-alkyl, (C1-C7)-alkoxy-group, halogen atom or trifluoromethyl; X means oxygen (O), sulfur (S) atom or two hydrogen atoms not forming a bridge; A1/A2 mean independently of one another phenyl or 6-membered heterocycle comprising 1 or 2 nitrogen atom; B represents group of the formula:

wherein R3 means (C1-C7)-alkyl and others; Y means -O-, -S- or a bond; Z means -O- or -S-; or B means 5-membered heterocyclic group of formulae: (a) , (b) , (c) or (d) . Also, invention relates to methods for preparing compounds and to a medicinal agent based on thereof.

EFFECT: improved preparing methods, valuable medicinal properties of compounds.

22 cl, 1 tbl, 2 sch, 78 ex

FIELD: organic chemistry, chemical technology, fungicides.

SUBSTANCE: invention describes derivative of benzoylpyridine of the formula (I) or its salt:

wherein X represents halogen atom, (C1-C6)-alkoxy-group optionally substituted with a substitute taken among halogen atom, phenyl, methoxy-, methylthio-, dimethylamino-group, vinyl or ethynyl; phenoxy-group, (C3-C6)-cycloalkoxy-group, hydroxyl group, (C1-C6)-alkyl group, (C2-C6)-alkenyl group, CF3, (C1-C6)-alkylthio-group, (C1-C6)-alkoxycarbonyl group, (C1-C6)-dialkylaminocarbonyl group, (C1-C6)-alkylcarbonyloxy-group, (C1-C6)-alkylcarbonyl group, amino-group, (C1-C4)-alkylamino-group or di-(C1-C4)-alkylamino-group; n represents 1, 2, 3 or 4; R1 represents (C1-C6)-alkyl group; R2 represents (C1-C6)-alkyl group, (C1-C6)-alkoxy-group optionally substituted with phenyl, phenoxy-group, (C3-C10)-cycloalkyloxy-group or hydroxyl group; m = 1, 2 or 3 under condition that if m = 2 then R2 can form ring -OCH2O- (with exception when pyridine ring is substituted with benzoyl group at 2-position; pyridine ring is substituted with (C1-C6)-alkoxy-group, hydroxyl group or benzyloxy-group; n = 1; m = 1 or 2). Also, invention describes fungicide comprising compound of the formula (I) or it salt as an active component, methods for preparing derivatives of benzoylpyridine, phenylpyridylmethanol that is an intermediate compounds used for synthesis of compound of the formula (I). Invention provides fungicide properties of compound of the formula (I) or its salt.

EFFECT: improved method for preparing, valuable properties of compounds.

17 cl, 36 tbl, 4 ex

FIELD: organic chemistry, chemical technology.

SUBSTANCE: invention relates to the improved methods for preparing compounds of the formulae (I) and (II) or their salts wherein X represents halogen atom; Y represents halogen atom, halogenalkyl, alkoxycarbonyl or alkylsulfonyl; n = 0-3. Method for preparing compound of the formula (I) involves catalytic hydrogenation of compound of the formula (II) in the presence of a catalyst, such as palladium in solvent medium at temperature from 0°C to 60°C. Method provides preparing the end compounds with high yields (95-97%) and high purity degree due to minimization of by-side dehalogenation reaction of the parent reagents. Method for preparing compound of the formula (II) involves treatment of the corresponding derivative of 2-fluoro-derivative with the cyanide source in the presence of a catalyst, such as tetraalkyl ammonium salt in an aqueous solvent or without solvent at temperature from 10°C to 60°C. Method provides preparing the end compounds with high yields (80-90%), high purity (98%) at moderate temperatures.

EFFECT: improved preparing methods.

23 cl, 3 ex

FIELD: organic chemistry, chemical technology.

SUBSTANCE: invention relates to a method for preparing tetrachloropicolinic acid. Method involves interaction of 2-cyanopyridine with chlorine in presence of catalysts wherein phosphorus chlorides are used in the amount 2-60 weight % of the initial load of 2-cyanopyridine, and phosphorus oxychlorides also. The chlorination process is carried out in the melt at temperature 120-200°C and under pressure up to 0.6 MPa followed by dosing the reaction mass into a mixture of water with sulfuric acid, and then hydrolysis is carried out in the presence of phosphoric acid formed after hydrolysis of phosphorus chlorides. The end product is isolated by the known procedures. Method provides simplifying the process by using the standard equipment, improving ecological indices and reducing energy consumptions.

EFFECT: improved preparing method.

2 cl, 6 ex

FIELD: organic chemistry, chemical technology.

SUBSTANCE: invention proposes a method for preparing 3,4,5,6-tetrachloro-2-cyanopyridine by interaction of 2-cyanopyridine with chlorine in the presence of phosphorus chlorides as a catalyst taken in the amount 2-60 weight % of the initial loads of 2-cyanopyridine. The chlorination process is carried out in the melt at temperature 120-200°C and under pressure up to 0.6 MPa. Method provides simplifying the process by using the standard equipment, improving ecological indices and decreasing energy consumptions.

EFFECT: improved preparing method.

3 cl, 8 ex

FIELD: chemical technology.

SUBSTANCE: method for preparing tetrachloropicolinic acid involves interaction of 2-cyanopyridine and chlorine in liquid phase in the melt at temperature 120-200°C under pressure up to 0.6 MPa in the presence of catalysts wherein phosphorus chlorides and oxychlorides are used in the mole ratio of 2-cyanopyridine to catalyst = 1:(0.1-1.0) followed by dissolving the reaction mixture in inert solvent, addition of water at temperature 70-80°C, decomposition of phosphorus chlorides at increased temperature to yield hydrogen chloride and phosphoric acid, separation of phosphoric acid from organic layer and the following addition of sulfuric acid to organic layer and hydrolysis of residue by heating the mixture to 120-140°C. Method provides increasing yield and purity of the end product, simplifying technology, reducing cost for its preparing.

EFFECT: improved preparing method.

2 cl, 5 ex

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to 2-hetaryl-substituted derivatives of 1,2-tropolones of the general formula (Ia): wherein R1 and R2 mean (C1-C6)-alkyl; R3 means hydrogen atom, (C1-C6)-alkyl, nitro-group; Het means six-membered nitrogen heterocycle condensed with one or two benzyl rings that can be substituted with substitutes chosen from group comprising halogen atom, nitro-group, (C1-C6)-alkyl, oxy-(C1-C6)-alkyl, secondary amino-group chosen from anilino-, substituted anilino-, hydroxyethylamino-group, or tertiary amino-group chosen from morpholino-, piperidino-, piperazino-group, 1H-1-imidazolyl. Also, invention relates to a method for synthesis of 2-hetaryl-substituted derivatives of 1,3-tropolone. Method involves condensation of benzoquinones-1,2 with 2-methylheterocycles at heating in the presence of acetic acid taken in the amount providing its role as both a catalyst and a solvent. Also, invention relates to a pharmaceutical composition with antibacterial effect based on 2-hetaryl-substituted derivatives of 1,3-tropolone.

EFFECT: improved method of synthesis, valuable medicinal properties of compounds and pharmaceutical composition.

9 cl, 5 tbl, 3 ex

FIELD: organic chemistry, fungicides.

SUBSTANCE: invention describes compound of the general formula (I): wherein p means a whole number = 1, 2, 3 or 4; q means a whole number = 1, 2, 3, 4 or 5; Each substitute X is chosen independently from halogen atom or linear or branched halogenalkyl comprising from 1 to 5 carbon atoms and wherein at least one substitute represents halogenalkyl; each substitute Y is chosen from halogen atom, alkyl, alkenyl, halogenalkyl, alkoxy-, halogenalkoxy-, alkylthio-group, alkoxycarbonyl, alkylamino-group, halogenthioalkyl, alkylsulfonyl, alkoxyalkenyl wherein each among alkyl radical means a linear or branched radical and comprises from 1 to 5 carbon atoms, amino-, cyano-, hydroxy-group, benzyl, halogensulfonyl, nitro-group, its N-oxide of 2-pyridine fragment with exception for N-{2-[3-chloro-5-(trifluoromethyl)-2-pyridinyl]ethyl}-2,6-dichlorobenzamide, and a method for its synthesis. Also, invention describes a fungicide composition and method for prophylactic or curative suppression of phytopathogenic fungi with using compound of the formula (I). Compound of the formula (I) possesses fungicide activity.

EFFECT: valuable properties of compound and fungicide composition.

15 cl, 2 tbl, 7 ex

FIELD: chemistry.

SUBSTANCE: new compounds with formula Ia are proposed, where: P represents pyridine or pyrimidine; R1 represents hydrogen; R2 is chosen from halogen, nitro, C0-6alkylheteroaryl, (CO)OR4, trifluoromethyl, C0-6alkylcyano, C0-6alkylNR4R5, OC1-6alkylNR4R5, C0-6alkylCONR4R5, C0-6alkyl(SO2)NR4R5 and X1R6 group, where X1 represents a direct link; R6 represents a 5- or 6-member heterocyclic group, containing one or two heteroatoms, independently chosen from N, O, and S, for which the given heterocyclic group can be unsaturated and can be substituted with by one substitute, chosen from W; m equals 0, 1, or 2; R3 is chosen from CO(OR4), C0-6alkylNR4R5, C0.6alkylCONR4R5, OC1-6alkylNR4R5 C1-6alkyl(SO2)NR4R5; n equals 1 or 2; R4 is chosen from hydrogen, C1-6alkyl; R5 is chosen from hydrogen, C1-6 alkyl, C0-6 alkyl C3-6 cycloalkyl, C0-6 alkylaryl, C0-6alkylheteroaryl and C1-6alkylNR14R15 or R4 and R5 together can form a 4-, 5-, 6- or 7-member heterocyclic group, containing one or more heteroatoms, independently chosen from N and O, where the given heterocyclic group can be substituted by group Y; and where any C1-6alkyl, indicated in defining R2-R5, can be substituted with one or more one Z group; R14 and R15 together can form a 5-member heterocyclic group, containing one or more heteroatoms, independently chosen from N and O; W and Z are independently chosen from halogen, CN, OR16, C1-6alkyl, trifluoromethyl, trifluoromethoxy, 5-member heterocyclic group, containing one heteroatom, independently chosen from N, for which the given heterocyclic group can be substituted with group Y; Y is chosen from oxo, halogen, C1-6alkyl, C0-6alkylaryl, NR16R17, phenyl, C0-6alkylaryl, where the phenyl and C0-6alkylaryl groups can be substituted with nitro, trifluoromethyl; R16 and R17 are independently chosen from hydrogen and C1-6alkyl, or where R16 and R17 together can form a 5-member heterocyclic group, containing one heteroatom, chosen from N; in form of a free base or pharmaceutical salt. Formula Ia compounds have inhibiting effect to glycogen-synthase-kinase-3 (GSK3). The invention also relates to the method of obtaining the proposed compounds and to new intermediate compounds, used in them, pharmaceutical compositions, containing the given therapeutically active compounds, and use of the given active compounds in therapy for treating conditions, related to GSK3.

EFFECT: new method of obtaining indole derivatives.

33 cl, 1 tbl, 112 ex

FIELD: organic chemistry, chemical technology.

SUBSTANCE: invention relates to derivatives of adamantine, in particular, to a new method for preparing adamant-1-yl-containing azoles of the general formula I-VIII: wherein R1 means ; R2 means ; R3 means ; R4 means ; R5 means ; R6 means ; R7 means , and R8 means . Indicated derivatives of adamantine are semifinished products used in synthesis of biologically active substances. Proposed method for preparing these compounds involves using a new method for synthesis of adamant-1-yl-containing azoles that includes the addition reaction of azoles: 2-methylimidazole, 3(5)-methylpyrazole and 4-methylpyrazole, 3,4-dinitropyrazole, 1,2,4-triazole, 3-methylpyrazole, 3-nitro-1,2,4-triazole and 5-methyltetrazole to 1,3-dehydroadamantane in the mole ratio of 1,3-dehydroadamantane to azole = 1:1 in diethyl ether medium at temperature 100°C for 4-5 h.

EFFECT: improved preparing method.

8 ex

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to using phenylethenyl- or phenylethynyl-derivatives as antagonists of glutamates receptors. Invention describes using compound of the general formula (I):

wherein each among R1, R2, R3, R4 and R5 means independently of one another hydrogen atom, (C1-C6)-alkyl, -(CH2)n-halogen, (C1-C6)-alkoxy-group, -(CH2)n-NRR', -(CH2)n-N(R)-C(O)-C1-C6)-alkyl, phenyl or pyrrolyl that can be unsubstituted or substituted with one or more (C1-C6)-alkyl; each among R, R' and R'' means independently of one another hydrogen atom or (C1-C6)-alkyl; A means -CH=CH- or C≡C; B means ,, , , or wherein R6 means hydrogen atom, (C1-C)-alkyl, -(CH2)n-C(O)OR, or halogen atom; R7 means hydrogen atom, (C1-C6)-alkyl, -(CH2)n-C(O)OR', halogen atom, nitro-group or oxodiazolyl group that can be unsubstituted or substituted with (C1-C6)-alkyl or cycloalkyl; R8 means hydrogen atom, (C1-C6)-alkyl, -(CH2)n-OH, -(CH2)n-C(O)OR'' or phenyl; R9 means (C1-C6)-alkyl; R10 and R11 mean hydrogen atom; R12 means -(CH2)n-N(R)-C(O)-(C1-C6)-alkyl; R13 means hydrogen atom; each R14, R15, R16 and R17 independently of one another means hydrogen atom or (C1-C6)-alkoxy-group; each R18, R19 and R20 independently of one another means hydrogen atom; R21 means hydrogen atom or (C1-C6)-alkyl; R22 means hydrogen atom, (C1-C6)-alkyl or (C1-C6)-alkyl comprising one or more substitutes chosen from groups hydroxy- or halogen atom; R23 means hydrogen atom, (C1-C6)-alkanoyl or nitro-group; each among R24, R25 and R26 independently of one another means hydrogen atom or (C1-C6)-alkyl; n = 0, 1, 2, 3, 4, 5 or 6; X means -O- or -S-; Y means -CH= or -N=, and its pharmaceutically acceptable salts used in preparing medicinal agents designates for treatment or prophylaxis of disorders mediated by mGluR5-receptors. Also, invention describes compounds of the formula (I-A), compound of the formula (I-B-1) given in the invention description, and a medicinal agent used in treatment or prophylaxis of disorders mediated by mGluR5-receptors.

EFFECT: valuable medicinal properties of compounds.

44 cl, 1 tbl, 44 ex

FIELD: chemistry of organophosphorus compounds, chemical technology.

SUBSTANCE: 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.

EFFECT: improved method of synthesis.

18 cl, 19 ex

FIELD: chemistry.

SUBSTANCE: invention relates to new displaced heterocyclic derivatives that can be used in treatment of diabetes and to reduce the content of cholesterol. In formula m is 1; n is 1; Q is C; A is -(CH2)x2-0-(CH2)x3-, where x2 varies from 1 to 3 and x3 is 0; B is a bond or it is (CH2)x4, where x4 varies from 1 to 2; X represents CH or N; X2, X3, X4, X5, X6 represent C, N, O; provided that one from X2 X3 X4 X5 and X6 represents N; and at least one of X2, X3, X4, X5, and X6 represents C; R1 represents H or C1-C6alkyl; R2 is H; R2a, R2b and R2c can be equal or different and selected from H, C1-C6alkyl, C1-C6alkoxy, halogen or thyano; R3 is selected from phenyloxycarbonile, C1-C6alkyloxycarbonile, phenylcarbinol, phenyl, alkoxy; Y represents CO2R4 (where R4 represents H or C1-C6alkyl); (CH2)m can be not necessarily displaced by 1 substitute.

EFFECT: produced are pharmaceutical composition for treatment of diabetes and to reduce the content of cholesterol.

13 cl, 2 tbl, 22 dwg, 88 ex

FIELD: chemistry.

SUBSTANCE: invention refers to synthesis of [18F]fluororganic compounds ensured by reaction of [18F]fluoride and relevant halogenide or sulphonate with alcoholic vehicle of formula 1 where R1, R2 and R3 represent hydrogen atom or C1-C18 alkyl.

EFFECT: possibility for mild process with low reaction time and high yield.

21 cl, 2 tbl, 27 ex

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