Uniformly marked with tritium tilosin
FIELD: chemistry; medicine.
SUBSTANCE: inventions relate to novel marked with tritium analogue of physiologically active compound- uniformly marked with tritium tylosin of formula: . Said compound is drastic antibiotic.
EFFECT: extension of assortment of marked analogues of physically active compound, which are applied in organic chemistry, in biology and in medicine.
1 cl, 1 dwg, 1 ex
The invention relates to the field of organic chemistry and can find application in analytical chemistry, Bioorganic chemistry, biochemistry and applied medicine.
For the study of physiologically active compounds that are necessary for their labeled counterparts.
It is known that the replacement compounds for their labeled counterparts does not change any properties of the original compound (E.A. Evans - Tritium and its compounds London Butterworths, 1974, p.48) .
Known tylosin formula
This compound is a highly effective antibiotic (J.W.Corcoran et al., J. Antibiot. 30, 1012 (1977)) .
However, tritium-labeled analogue not described.
The technical result achieved by the present invention, is expanding the range labeled analogs of the physiologically active substances.
Achieved the specified technical result obtaining a new labeled physiologically active compound is uniformly labeled with tritium tylosin.
The drawing shows the distribution of radioactivity and optical absorption at a wavelength of 280 nm in the analysis of labeled tylosin after the first stage of purification. Analysis conditions: column Reprosil pur C18aq, 5 μm, 4*150 mm, elution conditions:
|Eluent And||Meon-50 mm NH4H2PO4H 2.8, (6:4)|
|Gradient||Linear from 0 to 25% solvent b for 10 min|
|isocratic plot 25% eluent|
|10 to 15 min, flow of eluent 1|
|Retention time labeled tylosin||5.52 min|
The following is an example implementation of the invention
In the first chamber of the reaction dvukhmernoi ampoules were placed 10 µmol tylosin, 20 mg of palladium oxide and 25 mg of 5% PdO/BaSO4in the second 200 ál of absolute dioxane and 5 μl of triethylamine. The second camera was frozen with liquid nitrogen and the vial was evacuated to a pressure of 0.1 PA and filled with gaseous tritium to pressure 333 hPa. Then, the first chamber was heated to 70°C. the palladium Oxide was recovered tritium water was peremarazhival the second chamber of the Reaction, the ampoule was evacuated to a pressure of 0.1 PA, continuing to heat the first vial to 70°C and filled with argon. Then the contents of the second chamber was poured into the first chamber, which was sealed. Thus, the reaction mixture consisted of the recovered catalyst, 100% Tr is tavoy water, of triethylamine and a solution of tylosin in dioxane. The contents of the ampoules were heated for 20 min at 150°C. Then, the ampoule was opened, tritium water, triethylamine and dioxane drove under vacuum in a special receiver, the residue was dissolved in 3 ml of methanol and the catalyst was separated by filtration. The catalyst was washed with methanol (5×1 ml). Labile tritium was removed several times, dissolving the obtained labeled tylosin in methanol (5×2 ml) and pariva last.
The first stage of cleaning labeled tylosin was performed by HPLC (Kromasil column 100C 18.8×150 mm, flow rate 2 ml/min system: a mixture of methanol with ammonium phosphate buffer, pH 2.8, 6:4, the retention time of 7.2 min). Analysis of labeled tylosin after the first purification was performed by HPLC (radiochemical purity of about 70%) (see drawing).
The chromatogram shows two channels: the absorption of the eluent at a wavelength of 215 nm (UV215) and radioactivity eluent (Rad). Both channels are expressed in relative units (mV, directly generated by the detectors). On the chromatogram overlay profile gradient - concentration of eluent B (0→25%).
The drawing shows the change in optical absorbance and radioactivity by chromatography of the reaction mixture formed after the introduction of tritium label and see that tylosin contains tritium label and well separated from the isomeric products. Therefore, after the Torno purification of the obtained product with a radiochemical purity of 97-99%.
Before further treatment and after the final cleaning labeled tylosin eluent was absoluely. To do this, the solution labeled tylosin in eluent under reduced pressure to remove methanol, and then labeled tylosin was adsorbing on the cartridge Sep-Pack C18infiltrated water solution, and then the cartridge was washed with 2 ml water and washed labeled tylosin 3 ml of methanol.
Re-purification of labeled tylosin was performed by HPLC on the same column as the primary, but the following gradient conditions:
|Eluent And||Meon-50 mm NH4H2PO4pH 2.8, (6:4)|
|Gradient||Linear from 0 to 100% eluent b for|
|30 min, flow rate 2 ml/min|
|Retention time labeled tylosin||12.5 min|
For receiving and processing the chromatographic data were used hardware-software complex "Multichrome" (CJSC "ampersand character", Russia) based on IBM PC/AT. Radioactivity was measured by scintillation counter with an efficiency of registration of tritium 30% in dioxane scintillator.
About the rd output labeled drug after the second stage of treatment was 17%, molar radioactivity 5-7 CI/mol. Radiochemical purity of 97-99%.
Thus, the resulting new uniformly tritium-labeled physiologically active compound.
Uniformly labeled with tritium tylosin formula:
FIELD: organic chemistry, medicine, pharmacy.
SUBSTANCE: invention relates to compound of the formula (I) possessing inhibitory effect on production of interleukin-12 (IL-12) wherein R1 represents group of the formula , aryl or heteroaryl; each among R2 and R4 represents independently hydrogen atom, (C1-C6)-alkyl or (C1-C6)-alkoxy group; R3 represents Rc, alkenyl, -ORc, -OC(O)Rc, -SRc, -NRcCORd, -NRcC(O)ORd, -NRcC(O)NRcRd, -NRcSO2Rd, -CORc, -C(O)ORc or -C(O)NRcRd; R5 represents hydrogen atom (H); n = 0, 1, 2, 3, 4, 5 or 6; X represents oxygen atom (O) or -NRc; Y represents a covalent bond. -CH2, O or -NRc; Z represents nitrogen atom (N); one of values U and V represents N and another represents -CRc; W represents O, sulfur atom (S) or -S(O)2 wherein each radical among Ra and Rb represents independently H, (C1-C6)-alkyl, aryl or heteroaryl; each radical among Rc and Rd represents independently H, (C1-C6)-alkyl, phenyl, heteroaryl, cyclyl, heterocyclyl or (C1-C6)-alkylcarbonyl wherein term "aryl" relates to hydrocarbon cyclic system (monocyclic or bicyclic) comprising at least one aromatic ring; term "heteroaryl" relates to hydrocarbon cyclic system (monocyclic or bicyclic) comprising at least one aromatic ring that comprises at least one heteroatom, such as O, N or S as a part of cyclic system and wherein other atoms mean carbon; term "cyclyl" and "heterocyclyl" relate to partially or completely saturated monocyclic or bicyclic system comprising from 4 to 14 carbons in rings wherein heterocyclic ring comprises one or some heteroatoms (for example, O, N or S) as part of cyclic system and wherein other atoms mean carbon, and under condition that when X represents -NH, Y represents a covalent bond, n = 0, and R3 represents H or CH3 then R1 doesn't mean thiazolyl or pyrimidinyl. Also, invention relates to a pharmaceutical composition and a method for treatment of disorder associated with hyperproduction of interleukin-12.
EFFECT: valuable medicinal properties of compounds and pharmaceutical composition.
49 cl, 43 ex
FIELD: organic chemistry, medicine, oncology, pharmacy, biochemistry.
SUBSTANCE: invention relates to amide derivative represented by the following formula :
in any of the following cases (A) or (B), or its salt. In the case (A) R1 represents 5-7-membered saturated cyclic group comprising 1-2 nitrogen atoms as atom forming cycle (saturated cyclic amino-group can be substituted with 1-3 similar or different substitutes chosen from group consisting of (C1-C10)-alkyl, (C1-C10)-alkoxycarbonyl), mono-(C1-C10)-alkylamino- or di-(C1-C10)-alkylamino-group; R2 represents (C1-C10)-alkyl, halogen atom, halogen-(C1-C10)-alkyl, (C1-C10)-alkoxy-group, (C1-C10)-alkoxycarbonyl, nitro-group, mono-(C1-C10)-alkylcarbamoyl, di-(C1-C10)-alkylcarbamoyl or cyano-group; R3 represents hydrogen atom, halogen atom or (C1-C10)-alkoxy-group; Het1 represents any of the following formulae:  ,  ,  ,  ,  ,  and  ; Het2 represents pyridyl, pyrimidinyl, pyrazinyl or 1,2-dihydropyridazinyl (wherein Het2 can be substituted with 1-3 similar or different substitutes chosen from halogen atom) but except for compound wherein R1 means (i) pyrrolidinyl, piperidinyl, piperazinyl or morpholinyl and each of them can be substituted with 1-3 similar or different substitutes chosen from group consisting of alkyl, alkoxycarbonyl, halogen atom, halogenalkyl, hydroxyalkyl, amino-, monoalkylamino-, dialkylamino-group, carbamoyl, monoalkylcarbamoyl and dialkylcarbamoyl; (ii) monoalkylamino-group, or (iii) dialkylamino-group; Het1 means group of the formula , and Het2 means pyrazinyl or pyridyl and each of them can mean a substituted alkyl. In case the (B) R1 represents 4-methylpiperazin-1-yl, 1-pyrrolidinyl, piperidino-group, 4-ethylpiperazin-1-yl, 4-n-propylpiperazin-1-yl, cis-3,5-dimethylpiperazin-1-yl, morpholino-, dimethylamino- or diethylamino-group; R2 represents methyl, halogen atom, trifluoromethyl, methoxy-group, methoxycarbonyl, nitro-group, dimethylcarbamoyl or cyano-group; R3 represents hydrogen atom, bromine atom or methoxy-group; Het1 represents compound of the formula ; Het2 represents 3-pyridyl. Invention relates to a pharmaceutical composition possessing inhibitory activity with respect to BCR-ABL tyrosine kinase comprising amide derivative of the formula (I) or its salt as active component and a pharmaceutically acceptable nontoxic and inert carrier. Also, invention relates to BCR-ABL tyrosine kinase inhibitor, therapeutic agents comprising amide derivative of the formula (I) or its salt and, optionally, a pharmaceutically acceptable nontoxic and inert carrier used in treatment of chronic myelogenous leukemia, acute lymphoblast cell leukemia, acute myelogenous leukemia. Invention provides and proposes amide derivative inhibiting activity of BCR-ABL tyrosine kinase.
EFFECT: valuable medicinal properties of compounds and pharmaceutical composition.
8 cl, 2 tbl, 83 ex
FIELD: organic chemistry, chemical technology, medicine, pharmacy.
SUBSTANCE: invention relates to compounds of the formula (I)
or their pharmaceutically acceptable salts or esters hydrolyzing in vivo and possessing activity inhibiting the cellular cycle and selective with respect to CDK-2, CDK-4 and CDK-6. Compounds can be used in cancer treatment. In the formula (I) R1 represents halogen atom, amino-group, (C1-C)-alkyl, (C1-C6)-alkoxy-group; p = 0-4 wherein values R1 can be similar or different; R2 represents sulfamoyl or group Ra-Rb-; q = 0-2 wherein values R2 can be similar or different and wherein p + q = 0-5; R3 represents halogen atom or cyano-group; n = 0-2 wherein values R3 can be similar or different; R4 represents hydrogen atom, (C1-C6)-alkyl, (C2-C6)-alkenyl, (C2-C6)-alkynyl, (C3-C8)-cycloalkyl, phenyl or heterocyclic group bound with carbon atom wherein R4 can be optionally substituted at carbon atom with one or some groups Rd; R5 and R6 are chosen independently from hydrogen, halogen atom, (C1-C)-alkyl, (C2-C6)-alkenyl or (C3-C8)-cycloalkyl wherein R5 and R6 can be substituted at carbon atom independently of one another with one or some groups Re; Ra is chosen from (C1-C6)-alkyl, (C2-C6)-alkenyl, (C2-C6)-alkynyl, (C3-C8)-cycloalkyl, (C3-C8)-cycloalkyl-(C1-C6)-alkyl, phenyl, heterocyclic group, phenyl-(C1-C)-alkyl or (heterocyclic group)-(C1-C6)-alkyl wherein Ra can be substituted optionally at carbon atom with one or some groups Rg and wherein if indicated heterocyclic group comprises residue -NH- then its nitrogen atom can be optionally substituted with group chosen from the group Rh; Rb represents -N(Rm)C(O)-, -C(O)N(Rm)-, -S(O)r-, -OC(O)N(Rm)SO2-, -SO2N(Rm)- or -N(Rm)SO2- wherein Rm represents hydrogen atom or (C1-C6)-alkyl, and r = 1-2. Also, invention relates to methods for synthesis of these compounds, a pharmaceutical composition, method for inhibition and using these compounds.
EFFECT: improved preparing method, valuable medicinal properties of compounds and pharmaceutical compositions.
24 cl, 3 sch, 166 ex
FIELD: organic chemistry, medicine, pharmacy.
SUBSTANCE: invention relates to new derivatives of isoquinoline carboxamide of the formula (I):
and to their pharmaceutically acceptable salts wherein R1 means hydrogen atom, hydroxy-group or -NHR2 wherein R2 means alkyl, arylalkyl, heterocyclylalkyl that comprises one or some heteroatoms taken among nitrogen, oxygen and sulfur atoms, cycloalkyl, alkylcarbonyl, cycloalkylcarbonyl, arylcarbonyl, heterocyclylcarbonyl that comprises one or some heteroatoms taken among nitrogen, oxygen and sulfur atoms, arylalkylcarbonyl, heterocyclylalkylcarbonyl that comprises one or some heteroatoms taken among nitrogen and oxygen atoms, alkyloxycarbonyl, arylalkyloxycarbonyl, heterocyclylalkyloxycarbonyl that comprises one or some heteroatoms taken among nitrogen atom, heterocyclyl that comprises one or some heteroatoms taken among nitrogen and sulfur atoms, alkylsulfonyl, arylsulfonyl or the group of the formula:
R3 and R4 mean alkyl independently of one another; R5 means alkyl; or R4 and R5 in common with carbon and sulfur atoms to which they are bound form a heterocycle; R6 means alkyl; R13 means hydrogen atom or the group of the formula:
R15 means aryl under condition that if R3, R4 and R5 form methyl, R6 forms tert.-butyl then R13 means hydrogen atom, and if R15 means phenyl then R2 doesn't mean benzyloxycarbonyl and 2-quinoline carbonyl (other values of radicals are given in cl. 1 of the invention claim). Also, invention relates to a medicinal agent based on these compounds used in treatment of HIV-mediated diseases. Invention provides preparing new compounds and a medicinal agent based on thereof in aims for treatment of HIV-mediated diseases.
EFFECT: valuable medicinal properties of compounds and medicinal agent.
14 cl, 11 tbl, 173 ex
FIELD: organic chemistry, pharmacy.
SUBSTANCE: invention relates to new substituted derivatives of pyrrole of the formula (I): wherein R1 and R1' mean independently hydrogen atom (H) or (lower)-alkyl, unsubstituted or substituted (lower)-alkoxy-group; R2 means hydrogen atom (H), nitro-group (-NO2), cyano-group (-CN), halogen atom, unsubstituted (lower)-alkyl or substituted with halogen atom or (lower)-alkoxy-group; R2' means thiazolyl, thiophenyl, isothiazolyl, furanyl and pyrazolyl that is unsubstituted or substituted with (lower)-alkyl, pyrimidinyl, unsubstituted morpholinyl, unsubstituted pyrrolidinyl and imidazolyl that is unsubstituted or substituted with (lower)-alkyl, unsubstituted piperidinyl or piperazinyl that is unsubstituted or substituted with (lower)-alkyl, or ethoxy-group substituted with imidazolyl, or its pharmaceutically acceptable salt. Compounds of the formula (I) inhibit cell proliferation in G2/M phase of mitosis that allows their using in the pharmaceutical composition.
EFFECT: valuable biological properties of compounds.
36 cl, 4 sch, 1 tbl, 21 ex
or its pharmaceutically acceptable salt, where Rrepresents a group of formula -(ALK)q-R1where (ALK) represents alkyl, alkenyl or quinil, q is 0 or 1, R1represents a group of formula-CO2R2where R2is hydroxyalkyl, alkoxyalkyl or toolboxitem, Rrepresents a group of the formula
where o is 0 or 1, n is 0, 1 or 2, X represents N or CH, Y is O, NR11or CHR11where R11represents hydrogen, alkyl, hydroxyalkyl, alkoxyalkyl, carboxyl, or acyl, or a group of the formula -(alkyl)p-CN, -(alkyl)p-aryl, -(alkyl)p-O-aryl, -(alkyl)p-O-aralkyl, -(alkyl)p"heterocycle", -(alkyl)p-CO2"heterocycle" or -(alkyl-CO2)s-(alkyl)t-COR5and , in these formulas, R, s and t independently of each other 0 or 1, "heterocycle" represents a 5 the n heteroatom, represents a nitrogen, oxygen or sulfur, and which may substituted once or more than once, by substituents selected from the group consisting of halogen, alkyl and oxo, R5represents a hydroxy, alkoxy, hydroxy-C1-8-alkoxy, C1-8-alkoxyalkane, Tiltonsville, aryl, or aralkyl, or a group of the formula-NR6R7or-O-alkyl-NR6R7and , in these formulas, R6and R7independently of one another represent hydrogen or alkyl, and R14and R15independently of one another represent hydrogen, alkyl, hydroxyalkyl, alkoxyalkyl, carboxyl or acyl; or where R' is a group of formula -(ALK)q-R1where (ALK) represents alkyl, alkenyl or quinil, q is 0 or 1, R1represents fornillo group; and Rrepresents -(alkyl)m-CO2R8where m is 0 or 1, R8represents a group of formula -(alkyl)p-NR9R10where R is 0 or 1, and R9and R10together with the nitrogen atom to which they are attached, form a piperazinilnom group, possibly substituted by acyl
< / BR>where R1represents a methyl group, R2represents a methyl group, R4represents a hydroxy-group and X represents a methylene group; R1represents a methyl group, R2represents a hydrogen atom, R4represents a hydroxy-group and X represents a methylene group; R1represents a methyl group, R2represents a methyl group, R4represents a hydrogen atom and X represents a methylene group; R1represents a hydrogen atom, R2represents a hydrogen atom, R4represents a hydroxy-group and X represents a methylene group; or R1represents a methyl group, R2represents a methyl group, R4represents a hydroxy-group and X represents a sulfur atom
< / BR>whererepresents a single or double bond; R1represents a C1-C4alkyl; R2represents a C1-C4alkyl or C3-C6cycloalkyl; R1and R2together with the carbon atom to which they are joined, can form WITH3-C6cycloalkyl, optionally substituted stands; And represents СООR3CHO, CH2OH, COCH2HE, CONHCH2CH2OH, CONHOH or
R3hydrogen, C1-C12alkyl, which can be broken od is alkoxy, halogen, hydroxyl, C3-C6cycloalkyl, benzyloxy, fullam, phenyl, furfuryl, galopera, lower alkylphenyl, lower alkoxyphenyl, nitrophenyl, carboxyla, lower alkoxycarbonyl, cyano, C1-C4alkylthio or three (lower) alkylammonium; C3-C6alkenyl, optionally substituted by one of the following groups:1-C3alkoxy, phenyl, halogen or two WITH1-C3alkoxygroup or two halogen groups; C3-C6cyclooctyl, optionally substituted by one or two1-C3alkyl groups; C3-C10quinil, optionally substituted by phenyl, halogen or CH2IT; or the cation of an alkali metal or alkaline-earth metal (CA, BA) manganese, copper, iron, ammonium, or organic ammonium; RWITHand RDrepresent N or CH3; Represents N; COR4or SO2R5provided that when a represents a COR4or SO2R5and is a СOOR3the radical R3cannot be hydrogen or a salt-forming cation; R4represents a C1-C11alkyl, chloromethyl or phenyl, optionally substituted A5 alkyl or phenyl, optionally substituted one metalno, chloro - or nitro-group; W represents 0 or S; X represents 0, S or whenis a single bond, the group S 0; Y and Y', Z and Z' represent hydrogen, halogen, C1-C6alkyl, C1-C4hydroxy (lower) alkyl, C1-C6alkoxy, C1-C6acyloxy, benzoyloxy, optionally substituted by one or two1-C4alkyl, C1-C4alkoxygroup or halogen; C1-C4alkylthio, phenoxy,1-C4haloalkyl,1-C4haloalkoxy, nitro, cyano, C1-C4alkylamino,1-C4dialkylamino,1-C4alkylsulfonyl or phenyl, optionally substituted by one or more1-C4the alkyl, C1-C4alkoxy, halogen, or any combination of these two groups, where Y and Z are the same provided that Y and Z represent hydrogen, halogen, alkyl or alkoxy, and when Y and Y' or Z and Z' are the same group they are hydrogen or alkyl; and taken together, Y and Z form a ring in which YZ has the structural formula -(CH2)n- where n являе/www.fips.ru/fullimg/rupat2/19962/004.dwl/2058313-8t.gif" ALIGN="ABSMIDDLE">-=where L, M, Q, and R7each represent hydrogen, halogen, nitro, C1-C4lower alkyl, C1-C4lower alkoxy, methoxy, phenyl, phenoxy, provided that only one of the radicals L, M, Q or R7may have a value different from hydrogen, halogen, C1-C4the alkyl or C1-C4alkoxy; or a pyridine-N-oxides, when W represents oxygen or sulfur and a is COOR3; and when R1and R2not the same, the optical isomers of these compounds, except for the case when R3represents a salt-forming cation, their salts kislotoustoichivam
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
SUBSTANCE: present invention relates to biotechnology, more specifically to obtaining nucleoside-5'-triphosphates, labelled with phosphorous-32 (phosphorous-33) in the alpha-position, and can be used for analysis in molecular biology, genetics and medical biochemistry. The method is realised through treatment of labelled nucleosidephosphate in a buffer solution with a mixture of deoxyribonucleoside monophosphate kinase of bacteriophage T5 and pyruvate kinase with subsequent chromatographic purification of the target product.
EFFECT: simple method of obtaining nucleoside-5'-triphosphates and stable output of the target product.
SUBSTANCE: invention concerns compounds of the formula (Ia) and their application in radiological pharmaceutical compositions for linking to receptors associated with angiogenesis.
EFFECT: possible application in diagnostics or therapy, eg for malignant or cardiac diseases, endometriosis, inflammatory diseases, rheumatoid arthritis and sarcoma Kaposi.
SUBSTANCE: claimed invention relates to highly labelled by tritium [methyl-3H]methyltosylate of formula: . Compound can be used in synthesis of labelled by tritium compounds, which are used in biological research.
EFFECT: obtaining of highly labelled tritium.
5 ex, 4 dwg
SUBSTANCE: invention refers to production of new tritiated analogues of physiologically active compounds - triterpene glycosides of holothurians Cucumaria of formula: .
EFFECT: there are produced new tritiated analogues of physiologically active compounds.
2 cl, 2 ex
FIELD: medicine; pharmacology.
SUBSTANCE: new described α-hederin of formula: uniformly marked with tritium is actually analog of α-hederin - biologically active saponin.
EFFECT: new effective biological properties.
1 cl, 1 ex
FIELD: medicine; pharmacology.
SUBSTANCE: invention relates to the amyloid-binding compound or its water-soluble non-toxic salt, where Y is presented by NR1R2; Z means S; R1 is chosen from group consisting of H, methyl, propyl, (CH2)nOR' (where n = 1, 2 or 3 and R' is presented by H or by lowest alkyl group), CF3, CH2-CH2X, CH2-CH2-CH2X (where X = F, Cl, Br or I); where R2 is chosen from group consisting of lowest alkyl group, (CH2)nOR' (where n = 1, 2 or 3 and R' is presented by H or by lowest alkyl group), CF3, CH2-CH2X, CH2-CH2-CH2X (where X = F, Cl, Br or I); R3 - R10 are chosen independently from group, consisting of H, F, CI, Br, I, lowest alkyl group, (CH2)nOR' (where n = 1, 2 or 3) or OR' , and R' means H lowest alkyl group); provided, the compound isn't related one of the following compounds: methyl-[4-(6- methyl -benzothiazole-2-il)phenyl]amin, dimethyl -[4-(6- methyl - benzothiazole-2-il)phenyl]amin, and where at least one of R1-R10 substitutors contains the radioactive marker, chosen from group, which consists of 11C, 123I, 125I or 127I, and the described compounds don't contain the nitrogen quaternary atoms. The invented compounds are used for detection of the amyloid deposit in patient and in differential diagnostics of brain affected by Alzhemer's disease and normal brain. .
EFFECT: thioflavin derivatives are obtained for in vivo visualization and identification of amyloid deposit in patient.
16 cl, 2 tbl, 9 dwg, 9 ex
FIELD: organic chemistry, radiolabeled compounds.
SUBSTANCE: invention relates to tritium uniformly labeled [3H]-trans-3,7-dimethyl-9-(2,6,6-trimethyl-3-oxo-1-cyclohexene-1-yl)-2,4,6,8-nonatetraenic acid of the formula: . This compound is analog of physiologically active compound that can be used in organic chemistry, biology and medicine.
EFFECT: valuable properties of compound.
FIELD: organic chemistry, chemical technology.
SUBSTANCE: invention relates to an improved solid-phase method for synthesis of radioisotope indicators, in particular, for synthesis of compounds labeled with 18F that can be used as radioactive indicators for positron- emission tomography (PET). In particular, invention relates to a method for synthesis of indicator labeled with 18F that involves treatment of a precursor fixed on resin if the formula (I): SOLID CARRIER-LINKER-X-INDICATOR wherein X means a group promoting to nucleophilic substitution by a definite center of a fixed INDICATOR with 18F- ion for preparing a labeled indicator of the formula (II): 18F-INDICATOR; to compound of the formula (Ib):
and compound of the formula (Ih): ;
to radiopharmaceutical set of reagents for preparing indicator labeled with 18F for using in PET; to a cartridge for radiopharmaceutical set of reagents for preparing indicator labeled with 18F for using in positron-emission tomography.
EFFECT: improved method of synthesis.
13 cl, 1 sch, 3 ex
FIELD: organic chemistry, chemical technology.
SUBSTANCE: invention relates to a method for synthesis of saturated aliphatic carboxylic acids with stable carbon isotopes (1-13C). Method involves the hydrocarboxylation reaction of α-olefins with carbon monoxide (13CO) and water at temperature 100-170°C and under pressure not exceeding 5 MPa in the presence of a solvent and catalytic system containing palladium compound as complex PdCl2(PPh3)2 and triphenylphosphine PPh3 taken in the ratio from 1:2 to 1:100, respectively. Synthesized carboxylic acids can be used as diagnostic test-preparations in medicine practice and in criminology, scientific investigations and in other fields. Invention provides synthesis of enanthic acid and caprylic acid labeled by stable carbon isotope 13C at position 1 for a single step, to increase yield of acids as measured for isotope raw, to decrease cost price of acids and to obtain derivatives of (1-13C)-caprylic acid - (1-13C0-caprylate sodium and (carboxy-13C)-trioctanoine.
EFFECT: improved methods of synthesis.
9 cl, 6 ex
FIELD: organic chemistry, labeled compounds.
SUBSTANCE: invention relates to a new highly labeled compound that represent an analog of the known physiologically active compound that is the strongest toxin and inhibitor of some viable important processes, for example, sodium ions transporting. [3H]-Saxitoxin dihydrochloride highly labeled with tritium corresponds to the formula: .
EFFECT: valuable properties of compound.