发明公开
- 专利标题: PROCESS FOR PURIFICATION OF APREPITANT
- 专利标题(中): 程序对清洁阿瑞
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申请号: EP06796191.2申请日: 2006-08-28
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公开(公告)号: EP2057151A2公开(公告)日: 2009-05-13
- 发明人: PARTHASARADHI, Reddy, Bandi , RATHNAKAR REDDY, Kura , RAJI REDDY, Rapolu , MURALIDHARA REDDY, Dasari , SRINIVASA RAO, Thungathurthy
- 申请人: Hetero Drugs Limited
- 申请人地址: Hetero House 8-3-166/7/1, Erragadda Hyderabad, Andhrapradesh. Hyderabad 500 018 IN
- 专利权人: Hetero Drugs Limited
- 当前专利权人: Hetero Drugs Limited
- 当前专利权人地址: Hetero House 8-3-166/7/1, Erragadda Hyderabad, Andhrapradesh. Hyderabad 500 018 IN
- 代理机构: Thomas, Simon
- 国际公布: WO2008026216 20080306
- 主分类号: C07D413/06
- IPC分类号: C07D413/06
摘要:
The present invention relates to a process for obtaining pure aprepitant substantially free of undesired diastereomeric isomer, namely 5-[2(S)-[I (RS)- [3,5-bis(trifluoromethyl)-phenyl)ethoxy]-3-(S)-(4-fluorophenyl)-morpholin-4-yl- methyl]-3,4-dihydro-2H-1,2,4-triazol-3-one. The present invention further provides an improved process for preparation aprepitant crystalline form II. The present invention also relates to novel amorphous form of aprepitant, process for its preparation and to a pharmaceutical composition comprising it. The present invention further relates to aprepitant having mean particle size of less than about 11.5 microns, process for its preparation and to a pharmaceutical composition comprising it. Thus, for example, aprepitant having the content of diastereomeric impurity of 1.1 % is dissolved in ethyl acetate at 700C, the solution is concentrated to half the initial volume by distilling off ethyl acetate, and the resulting solid is collected at 0 - 50C to give pure aprepitant substantially free of diastereomeric impurity.
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