2-АМИНО-1-АРИЛ-5-(3,3-ДИМЕТИЛ-2-ОКСОБУТИЛИДЕН)-4-ОКСО-N-(ТИАЗОЛ-5-ИЛ)-4,5-ДИГИДРО-1Н-ПИРРОЛ-3-КАРБОКСАМИДЫ, ПРОЯВЛЯЮЩИЕ ПРОТИВООПУХОЛЕВУЮ И АНТИРАДИКАЛЬНУЮ АКТИВНОСТЬ, СПОСОБ ИХ ПОЛУЧЕНИЯ И ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ НА ИХ ОСНОВЕ
Государственное бюджетное образовательное учреждение высшего профессионального образования "Казанский государственный медицинский университет" Министерства здравоохранения и социального развития" (RU)
发明人:
Зыкова Светлана Сергеевна (RU),Бойчук Сергей Васильевич (RU),Игидов Назим Мусабекович (RU),Одегова Татьяна Федоровна (RU),Захматов Антон Викторович (RU),Галембикова Айгуль Рафиковна (RU),Рамазанов Бул
申请号：
RU2015117807
公开号：
RU2015117807A
申请日:
2015.05.12
申请国别(地区):
RU
年份:
2016
代理人:
摘要：
1. A compound of general formula I wherein R is a C6-C10 aryl optionally substituted with one or more halogen atoms, or a pharmaceutically acceptable soli.2. A compound according to Claim. 1, where R represents phenyl or naftil.3. A compound according to claim. 2, where the phenyl is substituted with one or more atoms galogena.4. A compound according to claim. 3, where the phenyl is substituted by one or two atoms broma.5. A compound according to claim. 3, where the phenyl is substituted by one or two atoms hlora.6. The compound of claim 1 which is a compound of formula 1a or 1b. 7. A compound according to any one of claims. 1-6 in a pharmaceutically acceptable soli.8. A compound according to claim. 7, wherein the pharmaceutical salt is a hydrochloride, phosphate or atsetat.9. A process for preparing a compound of general formula I wherein R is a C6-C10 aryl optionally substituted with one or more halogen atoms, or a pharmaceutically acceptable salt thereof, which comprises reacting 4-R-Amino-2-tert-butyl-2,5-dihydro-5 -oksofuran-2-yl acetate (III) and 2-cyano-N- (thiazol-2-yl) acetamide in the presence of triethylamine, according to the following scheme: 10. A method according to claim. 9, wherein the 4R-amino-2-tert-butyl-2,5-dihydro-5-oksofuran-2-yl acetate (III) and 2-cyano-N- (thiazol-2-yl) acetamide take in equimolar kolichestve.11. The method of claim. 10 or 9, wherein triethylamine employed in an amount from equimolar to two-fold excess with respect to the 2-cyano-N- (thiazol-2-yl) acetamide 4R-2-tert-butyl-2,5-dihydro- 5-oksofuran-2-ilatsetatu.12. The method of claim. 10 or 9, wherein the reaction is carried out in benzola.13 medium. The method of claim. 12 wherein the resulting product of formula I compound precipitates as osadka.14. The method of claim. 12 wherein perekristallizovyvayut.15 precipitate. The method of claim. 14 wherein the solvent used for the recrystallization or benzene etanol.16. Pharmaceutical composition1. Соединение общей формулы Iгде
