公开(公告)号：EP1968934A1

公开(公告)日：2008-09-17

申请号：EP06711349.8

申请日：2006-01-02

申请人： Hetero Drugs Limited

发明人： PARTHASARADHI, Reddy, Bandi ,  RATHNAKAR, Reddy, Kura ,  RAJI, Reddy, Rapolu ,  MURALIDHARA, Reddy, Dasari ,  SUBASH CHANDER REDDY, Kesireddy

IPC分类号： C07C231/22

CPC分类号： C07C231/12 ,  C07C231/24 ,  C07C2601/16 ,  C07C233/52

摘要： The present invention provides a process for obtaining highly pure crystalline form of oseltamivir free base, thus, for example, suspending or dissolving impure or non-crystalline oseltamivir free base in a hydrocarbon solvent and then isolating crystals to obtain oseltamivir free base in well defined crystalline form. The present invention also provides a process for preparation of oseltamivir phosphate in high purity.

摘要翻译： 本发明提供了一种获得奥司他韦游离碱的高纯度结晶形式的方法，因此例如将不纯的或非结晶的奥司他韦游离碱悬浮或溶解在烃溶剂中，然后分离晶体以获得明确定义的结晶中的奥司他韦游离碱 形成。 本发明还提供了一种制备高纯度磷酸奥司他韦的方法。

公开(公告)号：EP2057151A2

公开(公告)日：2009-05-13

申请号：EP06796191.2

申请日：2006-08-28

申请人： Hetero Drugs Limited

发明人： PARTHASARADHI, Reddy, Bandi ,  RATHNAKAR REDDY, Kura ,  RAJI REDDY, Rapolu ,  MURALIDHARA REDDY, Dasari ,  SRINIVASA RAO, Thungathurthy

IPC分类号： C07D413/06

CPC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.