METHOD OF PRODUCING ETHYL ETHER OF 6-BROMO-5-HYDROXY-4-DIMETHYL AMINOMETHYL-1-METHYL-2-PHENYLTHIOMETHYLINDOLE-3-CARBOXYLIC ACID HYDROCHLORIDE MONOHYDRATE IN α-CRYSTALLINE FORM Russian patent published in 2012 - IPC C07D209/42 

FIELD: chemistry.

SUBSTANCE: invention relates to a novel α-crystalline form of ethyl ether of 6-bromo-5-hydroxy-4-dimethyl aminomethyl-1-methyl-2-phenylthiomethylindole-3-carboxylic acid hydrochloride monohydrate, which is characterised by the following X-ray diffraction parameters

The invention also relates to a method of producing said compound, involving bromination of ethyl ether of 5-acetoxy-1,2-dimethylindole-3-carboxylic acid to obtain ethyl-5-acetoxy-6-bromo-2-bromomethyl-1-methylindole-3-carboxyl, alkylation thereof with thiophenolate of an alkali metal at temperature 15-60°C for 1-2 hours, to obtain ethyl ether of 6-bromo-5-hydroxy-1-methyl-2-phenylthiomethyl-indole-3-carboxylic acid, aminomethylation thereof with dimethylamine to obtain ethyl ether of 6-bromo-5-hydroxy-4-dimethyl aminomethyl-1-methyl-2-phenylthiomethylindole-3-carboxylic acid with subsequent conversion of the obtained compound to a hydrochloride monohydrate and recrystallisation from ethanol or a mixture of ethanol and acetone.

EFFECT: improved method.

7 cl, 3 dwg, 6 ex