BRASKA Mariya Gabriella,БРАСКА Мария Габриелла,BANDERA Titsiano,БАНДЬЕРА Тициано,BERTRAN Dzhej Aaron,БЕРТРАН Джей Аарон,NOKKI Paola,НЬОККИ Паола,MIRITSTSI Danilo,МИРИЦЦИ Данило,NEZI Marchella,НЕЗИ Мар
申请号：
RU2013151174
公开号：
RU0002621732C2
申请日:
2012.04.05
申请国别(地区):
RU
年份:
2017
代理人:
摘要：
FIELD: chemistry.SUBSTANCE: substituted pyrimidinyl pyrrole compounds or pharmaceutically acceptable salts thereof are selected from the group consisting of 5-(2-aminopyrimidin-4-yl)-2-[2-chloro-5-(trifluoromethyl) phenyl]-1H-pyrrole-3-carboxamide, 5-(2-aminopyrimidin-4-yl)-2-(2,5-dichlorophenyl)-1H-pyrrole-3-carboxamide, 5-(2-aminopyrimidin-4-yl)-2-(5-chloro-2-ethylphenyl)-1H-pyrrole-3-carboxamide, 5-(2-minopyrimidin-4-yl)-2-[2-ethyl-5-(trifluoromethyl)phenyl]-1H-pyrrole-3-carboxamide, 5-(2-aminopyrimidin-4-yl)-2-(5-chloro-2-ethylphenyl)-N-methyl-1H-pyrrole-3-carboxamide, 5-(2-aminopyrimidin-4-yl)-2-(5 chloro-2-ethylphenyl)-N-ethyl-1H-pyrrole-3-carboxamide, 5-(2-aminopyrimidin-4-yl)-2-[2-chloro-5-(trifluoromethyl)phenyl]-N-methyl-1H-pyrrole-3-carboxamide, 2-(5-chloro-2-methylphenyl)-5-[2-(methylamino)pyrimidin-4-yl]-1H-pyrrole-3-carboxamide and 5-(2-aminopyrimidin-4-yl)-2-[2-ethyl-5-(trifluoromethyl)phenyl]-N-methyl-1H-pyrrole-3-carboxamide. The invention also relates to versions of the method for preparation of these compounds. For example, the method may include the steps (1): metal-catalyzed coupling reaction of a halogenated derivative of formulawith a substituted phenylboronic acid of formulaor henylboronic acid ester of formula,(2) alkaline hydrolysis of the obtained carboxylic acid ester of formula(3) amidation of the obtained carboxylic acid ester of formulaby a reaction with a derivative of formula (VI) NHR8R9, to obtain a compound of formulawherein R1, R2, R3, R4, R8 and R9 values are given in the claims, and R12 is hydrogen and if desired, convertion of a compound of formula (I) to a pharmaceutically acceptable salt or salt convertion to the free compound (I). Method versions include amidation of the carboxylic acid ester of formula (IV) without carboxylic acid (V) isolation or direct preparation of formula I compound without isolation of the intermediate compound of formula (IV) and (V). To prepare the formula I compound, where R12 is hydrogen, the meth
