Закрытое акционерное общество "Активный Компонент" (RU)
发明人:
Шкляренко Артем Александрович (RU),Логвинов Александр Владимирович (RU),Корчевская Елена Владимировна (RU),Булатова Анна Вадимовна (RU)
申请号：
RU2014152556
公开号：
RU2014152556A
申请日:
2014.12.24
申请国别(地区):
RU
年份:
2016
代理人:
摘要：
1. Industrial process for the preparation of pharmaceutical troventola comprising Oxymethylation tropine ester of 2-phenylbutyric acid paraformaldehyde, extraction of the resulting byproducts, isolation tropine ester of 2-hydroxymethyl-2-phenylbutyric acid, followed by quaternization with methyl iodide it, characterized in that the ester Oxymethylation Tropinova 2 -fenilmaslyanoy acid is carried out in dimethylacetamide solution at a ratio of 1: 1-1: 1.5 and a temperature of 20-25 ° C in the presence of potassium tert-butoxide, the reaction mass is added a weak sol p hydrochloric acid, by-products were extracted with ethyl acetate, and tropine ester of 2-hydroxymethyl-2-phenylbutyric acid was isolated by precipitation with carbonates, alkali metal followed by recrystallization from acetonitrile and tropine quaternized ester of 2-hydroxymethyl-2-phenylbutyric acid in acetonitrile solution, wherein troventola isolated crystals with a melting point of 263 ° C (decomp.) and a purity of more than 99.5% .2. Industrial process according to claim. 1, characterized in that the reaction by-products are removed by extraction uglevodorodami.3. Industrial process according to claim. 2, characterized in that the hydrocarbon used as geptan.4. Industrial process according to claim. 2, characterized in that the hydrocarbon used as toluol.5. Industrial process according to claim. 1, characterized in that as alkali metal carbonate is used natriya.6 carbonate. Industrial process according to claim. 1, characterized in that as alkali metal carbonate, potassium carbonate is used.1. Промышленный способ получения фармакопейного тровентола, включающий оксиметилирование тропинового эфира 2-фенилмасляной кислоты параформом, экстракцию образующихся побочных продуктов, выделение тропинового эфира 2-гидроксиметил-2-фенилмасляной кислоты, а затем его кватернизацию йодистым метилом, отличающийся тем, что оксиметилирование тропинового эфира 2-фенилмасляной кислоты проводят в растворе диметилацетами
