发明授权
US08937053B2 Process for the preparation of prasugrel and several novel crystalline forms of prasugrel hydrochloride
有权
制备普拉格雷和几种新型的普拉格雷盐酸盐结晶形式的方法
- 专利标题: Process for the preparation of prasugrel and several novel crystalline forms of prasugrel hydrochloride
- 专利标题(中): 制备普拉格雷和几种新型的普拉格雷盐酸盐结晶形式的方法
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申请号: US14123109申请日: 2012-06-21
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公开(公告)号: US08937053B2公开(公告)日: 2015-01-20
- 发明人: Lijun Li , Hailong Wang , Zhongqing Wang
- 申请人: Lijun Li , Hailong Wang , Zhongqing Wang
- 申请人地址: CN Dongguan, Guangdong CN Yidu,Hubei
- 专利权人: Sunshine Lake Pharma Co., Ltd.,Yichang Changjiang Pharmaceutical Co., Ltd.
- 当前专利权人: Sunshine Lake Pharma Co., Ltd.,Yichang Changjiang Pharmaceutical Co., Ltd.
- 当前专利权人地址: CN Dongguan, Guangdong CN Yidu,Hubei
- 代理机构: Squire Patton Boggs
- 代理商 Kam W. Law
- 优先权: CN201110169901 20110622
- 国际申请: PCT/CN2012/077320 WO 20120621
- 国际公布: WO2012/175031 WO 20121227
- 主分类号: C07D491/02
- IPC分类号: C07D491/02 ; A61K31/695 ; C07F7/18 ; C07D495/04
摘要:
Disclosed herein are a process or method for the preparation of prasugrel and several novel crystalline forms of prasugrel hydrochloride. The process comprises preparation of prasugrel by acetylation in solvents which have low boiling point and/or low toxicity, and the process not only avoids using solvents which have high boiling point and/or high toxicity such as toluene, acetonitrile and so on, but also resolves the problem about thermal instability of prasugrel, and the loss of prasugrel is reduced, as well as the yield is raised. The yield of prasugrel is higher than 85% and the purity is higher than 99.5%. The process can prepare prasugrel and its pharmaceutically acceptable salts. The novel crystalline forms of prasugrel hydrochloride are crystalline form H1, H2 and H3, and their performance in oral absorbability, activating metabolism and inhibiting platelet aggregation is excellent. They have a low toxicity and good thermal stability, and are applicable to the preparation of a drug for preventing or treating diseases caused by thrombosis or embolism.
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