Nucleophilic fluorination in solid phase

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

 



 

Same patents:

FIELD: pharmaceutical technology.

SUBSTANCE: invention relates to the improved sucralose formulation and a method for its crystallization. Method involves controlling pH value of solution in the range from about 5.5 to about 8.5 in the process of formation of sucralose crystals. Invention provides the development of the improved composition comprising crystalline sucralose and possessing the enhanced stability.

EFFECT: improved preparing method, improved properties of composition.

24 cl, 4 tbl, 4 ex

The invention relates to medicine, more specifically to radiopharmaceuticals for diagnostic purposes, and may find application in positron emission tomography

The invention relates to the technology of 1,4 : 3,6-dianhydro-D-sorbitol (sorbed, isosorbide), which is an intermediate in the production of medicines on the basis of its mono - and dinitropropane, which is used as a vasodilator prolonged action in hypertension, angina and other cardiovascular diseases

The invention relates to the field of organic chemistry and relates to the process of obtaining intermediate for the synthesis of vitamin B2

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to geranyl compounds represented by the following formulas (I-1) , (I-2) or (I-3) wherein R1 means compounds of the following formulas: or R2 means a group remaining after removing all carboxyl groups presenting in carboxylic acid chosen from group consisting of malic acid, citric acid, succinic acid, fumaric acid and others; m = 1, 2 or 3; n = 0, 1 or 2, and m + n represent a number of carboxylic groups presenting in indicated carboxylic acid; R3 means p-hydroxyphenyl or mercapto-group. Also, invention relates to derivatives of mevalonic acid represented by the following formula (I-4): wherein R means -CH2OH or CH3. Also, invention to an antitumor agent comprising as an active component geranyl compound of formulas (I-1), (I-2) or (I-3) or derivative of mevalonic acid of the formula (I-4), and optionally a pharmaceutically acceptable carrier or solvent. Also, invention relates to a method for treatment of liver cancer based on using geranyl compound of formulas (I-1), (I-2) or (I-3), or derivative of mevalonic acid of the formula (I-4) and using proposed compounds in manufacturing an antitumor agent. Invention provides using geranyl compounds or derivatives of mevalonic acid as antitumor agents.

EFFECT: valuable medicinal properties of compounds and pharmaceutical composition.

7 cl, 3 tbl, 17 ex

FIELD: organic chemistry, chemical technology, medicine.

SUBSTANCE: invention relates to a method for preparing 1-isonicotinyl-2-D-glucosyl hydrazone. In the glucosylation reaction of isonicotinic acid hydrazide the method involves using anionite AN 31 GS as a catalyst of the enhanced effectiveness, and using 95-96.5% ethanol or 85-90% isopropanol as the reaction medium. At the final stage the method involves sorption of contaminating impurities with activated carbon followed by drying the end product in nitrogen atmosphere.

EFFECT: improved preparing method.

2 cl, 1 ex

FIELD: pharmaceutical technology.

SUBSTANCE: invention relates to the improved sucralose formulation and a method for its crystallization. Method involves controlling pH value of solution in the range from about 5.5 to about 8.5 in the process of formation of sucralose crystals. Invention provides the development of the improved composition comprising crystalline sucralose and possessing the enhanced stability.

EFFECT: improved preparing method, improved properties of composition.

24 cl, 4 tbl, 4 ex

The invention relates to a method of joining azide function to organic connection

The invention relates to new derivatives of fatty acids, which drugs or agrochemicals, with improved performance as it relates to lipophilic derivative of biologically active compounds of the General formula CH3-(CH2)7-CH=CH-(CH2)n-X -, where n is an integer of 7 or 9; X is selected from the group comprising-COO-, -CONH-, -CH2O-, -CH2S-, -CH2O-CO-, -CH2NHCO-, -COS-; lipophilic group SN3-(CH2)7-CH=CH-(CH2)n-X - is CIS - or transconfiguration; And is a fragment of a molecule of biologically active compounds (BAC), non-nucleoside and nucleoside derivative and containing in its structure at least one of functional groups selected from a) alcohol, b) simple broadcast) phenol, (d) amino, (e) thiol, (f) carboxylic acids and (g) of ester carboxylic acid, provided that no connection specified in paragraph 1 of the claims

The invention relates to N-allyl-D-glucosamine formula (1) as adaptogene

The invention relates to the field of organic chemistry and can find application in biology and medicine

The invention relates to organic chemistry and can be used in analytical and biological chemistry, applied medicine

FIELD: organic chemistry, antiviral agents.

SUBSTANCE: invention relates to a method for synthesis of β-L-5-fluoro-2',3'-dideoxy-2',3'-didehydrocytidine (β-L-FD4C) that is used as an antiviral agent. This method can be used in the large-scale manufacture of β-L-FD4C and it displays the effectiveness, high economy and ecology acceptable.

EFFECT: improved method of synthesis.

23 cl, 1 tbl, 1 ex

FIELD: radiolabeled compounds, biochemistry.

SUBSTANCE: invention relates to a novel labeled analogue of the physiologically active compound, namely, tritium-labeled acyl-coenzyme A of the general formula (I): wherein Acyl means [5,6-3H]-(5,6-dihydro)-arachidonoyl or [6,7-3H]-linoleyl.

EFFECT: valuable medicinal and biochemical properties of compound.

2 dwg, 4 ex

FIELD: medicine, pharmacology, bioorganic chemistry, pharmacy.

SUBSTANCE: invention relates to the effective using amount of β-L-2'-deoxynucleoside of the formula (I) or (II) used in manufacturing a medicinal agent used in treatment of hepatitis B, pharmaceutical compositions containing thereof, and methods for treatment of hepatitis B. Proposed agent shows the enhanced effectiveness in treatment of hepatitis B.

EFFECT: enhanced and valuable medicinal properties of agent.

83 cl, 6 tbl, 11 ex

FIELD: medicine, pharmacology, bioorganic chemistry, pharmacy.

SUBSTANCE: invention relates to the effective using amount of β-L-2'-deoxynucleoside of the formula (I) or (II) used in manufacturing a medicinal agent used in treatment of hepatitis B, pharmaceutical compositions containing thereof, and methods for treatment of hepatitis B. Proposed agent shows the enhanced effectiveness in treatment of hepatitis B.

EFFECT: enhanced and valuable medicinal properties of agent.

83 cl, 6 tbl, 11 ex

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