公开(公告)号：EP2467373A2

公开(公告)日：2012-06-27

申请号：EP10747476.9

申请日：2010-08-18

申请人： Cipla Limited

发明人： RAO, Dharmaraj Ramachandra ,  KANKAN, Rajendra Narayanrao ,  CHIKHALIKAR, Sandip Vasant ,  GHAGARE, Maruti

IPC分类号： C07D401/04 ,  A61K31/404 ,  A61K31/405

CPC分类号： C07D401/04 ,  Y02P20/55

摘要： The present invention relates to a process for preparing naratriptan or a salt thereof, the process comprising: (a) reacting a compound of formula (3) with a compound of the formula HCCR wherein Z is a protecting group, Y is a leaving group and R is a trialkyl silyl group, a trialkylstannyl group or a zinc (II) halide, to obtain the compound of formula (4); (b) converting the compound of formula (4) to a compound of formula (5) wherein Z' is hydrogen or a benzyl group; (c) converting the compound of formula (5) to naratriptan; and (d) optionally converting naratriptan to a salt thereof. The present invention also provides novel compounds (3) and (4) and processes for their preparation.

公开(公告)号：EP2768811A1

公开(公告)日：2014-08-27

申请号：EP12780256.9

申请日：2012-10-19

申请人： Cipla Limited

发明人： RAO, Dharmaraj Ramachandra ,  KANKAN, Rajendra Narayanrao ,  NAIK, Sanjay ,  GHAGARE, Maruti ,  CHIKHALIKAR, Sandip Vasant

IPC分类号： C07D239/34 ,  C07D239/46 ,  C07C69/00

CPC分类号： C12P7/62 ,  C07C67/313 ,  C07C69/716 ,  C07D239/34 ,  C07D239/46 ,  C12P17/12

摘要： The present invention relates to a novel process for the preparation of a compound of formula (I) wherein R is a methyl or methoxy group; to certain novel intermediates prepared in such a process and their use.

摘要翻译： 本发明涉及一种制备式（I）化合物的新方法，其中R是甲基或甲氧基; 对于在这种方法中制备的某些新型中间体及其用途。

公开(公告)号：EP2467373B1

公开(公告)日：2013-10-02

申请号：EP10747476.9

申请日：2010-08-18

申请人： Cipla Limited

发明人： RAO, Dharmaraj Ramachandra ,  KANKAN, Rajendra Narayanrao ,  CHIKHALIKAR, Sandip Vasant ,  GHAGARE, Maruti

IPC分类号： C07D401/04 ,  A61K31/404 ,  A61K31/405

CPC分类号： C07D401/04 ,  Y02P20/55

公开(公告)号：EP2307392A2

公开(公告)日：2011-04-13

申请号：EP09757761.3

申请日：2009-06-02

申请人： Cipla Limited

发明人： RAO, Dharmaraj Ramachandra ,  KANKAN Rajendra Narayanrao ,  GHAGARE, Maruti ,  CHIKHALIKAR, Sandip Vasant

IPC分类号： C07D295/088

CPC分类号： C07D295/096 ,  C07C217/58 ,  C07C309/66 ,  C07D295/073 ,  C07D295/088

摘要： The present invention provides a compound of formula (IV) wherein R is Cl, Br, NO
2 , OH or OR', and R' is alkyl, and its use in the synthesis of levocetirizine, including its use in the synthesis of (-)-1-[(4-chlorophenyl)-phenyl methyl] piperazine, an intermediate useful in the synthesis of levocetirizine. The present invention also provides compounds (II) and (III) which are useful in the synthesis of compound (IV).