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1. 发明申请

WO2009125430A3 IMPROVED PROCESS FOR PRODUCING DARIFENACIN 审中-公开
公开(公告)号：WO2009125430A3
公开(公告)日：2009-10-15
申请号：PCT/IN2009/000160
申请日：2009-03-09
申请人： MATRIX LABORATOIRES LIMITED , TYAGI, Om, Dutt , RAY, Purna, Chandra , CHAUHAN, Yogendhra, Kumar , RAO, K., Babu , REDDY, N., Mahhander , REDDY, D., Siva, Prasad
发明人： TYAGI, Om, Dutt , RAY, Purna, Chandra , CHAUHAN, Yogendhra, Kumar , RAO, K., Babu , REDDY, N., Mahhander , REDDY, D., Siva, Prasad
IPC分类号： C07D405/06
摘要： The present invention discloses an improved process for producing darifenacin, the process comprising decarboxylating (2S,4R)-4-hydroxy-2-pyrrolidine carboxylic acid followed by in situ tosylation to give l-tosyl-3-(R)-(-)-hydroxypyrrolidine, tosylating the l-tosyl-3-(R)-(-)-hydroxypyrrolidine with methyl-p-toluenesuolphonate to give l-tosyl-3- (S)-(-)-tosyloxy pyrrolidine, reacting l-tosyl-3-(S)-(-)-tosyloxy pyrrolidine with diphenyl acetonitrile in presence of a base to give 3-(S)-(+)-(l-cyano-l,l-diphenylmethyl)-l- tosylpyrrolidine, de-protecting 3-(S)-(+)-(l-cyano-l,l-diphenylmethyl)-l- tosylpyrrolidine in the presence of phenol in acidic medium to give 3-(S)-(+)-(l-cyano- 1,1-diphenylmethyl) pyrrolidine, hydrolyzing 3-(S)-(+)-(l-cyano-l,l-diphenylmethyl) pyrrolidine followed by salt formation to obtain 3-(S)-(+)-(l-carbamoyl-l,l- diphenylmethyl)pyrrolidine.L-(+)-tartrate, condensing 3-(S)-(+)-( 1 -carbamoyl- 1,1- diphenylmethyl)pyrrolidine-L(+)-tartrate with 5-(2-bromoethyl)-2,3-dihydrobenzofuran employing a base in a solvent to give darifenacin.

2. 发明申请

WO2009125430A8 IMPROVED PROCESS FOR PRODUCING DARIFENACIN 审中-公开
公开(公告)号：WO2009125430A8
公开(公告)日：2009-10-15
申请号：PCT/IN2009/000160
申请日：2009-03-09
申请人： MATRIX LABORATOIRES LIMITED , TYAGI, Om, Dutt , RAY, Purna, Chandra , CHAUHAN, Yogendhra, Kumar , RAO, K., Babu , REDDY, N., Mahhander , REDDY, D., Siva, Prasad
发明人： TYAGI, Om, Dutt , RAY, Purna, Chandra , CHAUHAN, Yogendhra, Kumar , RAO, K., Babu , REDDY, N., Mahhander , REDDY, D., Siva, Prasad
IPC分类号： C07D405/06
摘要： The present invention discloses an improved process for producing darifenacin, the process comprising decarboxylating (2S,4R)-4-hydroxy-2-pyrrolidine carboxylic acid followed by in situ tosylation to give l-tosyl-3-(R)-(-)-hydroxypyrrolidine, tosylating the l-tosyl-3-(R)-(-)-hydroxypyrrolidine with methyl-p-toluenesuolphonate to give l-tosyl-3- (S)-(-)-tosyloxy pyrrolidine, reacting l-tosyl-3-(S)-(-)-tosyloxy pyrrolidine with diphenyl acetonitrile in presence of a base to give 3-(S)-(+)-(l-cyano-l,l-diphenylmethyl)-l- tosylpyrrolidine, de-protecting 3-(S)-(+)-(l-cyano-l,l-diphenylmethyl)-l- tosylpyrrolidine in the presence of phenol in acidic medium to give 3-(S)-(+)-(l-cyano- 1,1-diphenylmethyl) pyrrolidine, hydrolyzing 3-(S)-(+)-(l-cyano-l,l-diphenylmethyl) pyrrolidine followed by salt formation to obtain 3-(S)-(+)-(l-carbamoyl-l,l- diphenylmethyl)pyrrolidine.L-(+)-tartrate, condensing 3-(S)-(+)-( 1 -carbamoyl- 1,1- diphenylmethyl)pyrrolidine-L(+)-tartrate with 5-(2-bromoethyl)-2,3-dihydrobenzofuran employing a base in a solvent to give darifenacin.

3. 发明申请

WO2009125430A2 IMPROVED PROCESS FOR PRODUCING DARIFENACIN 审中-公开
标题翻译：改进生产DARIFENACIN的方法
公开(公告)号：WO2009125430A2
公开(公告)日：2009-10-15
申请号：PCT/IN2009/000160
申请日：2009-03-09
申请人： MATRIX LABORATOIRES LIMITED , TYAGI, Om, Dutt , RAY, Purna, Chandra , CHAUHAN, Yogendhra, Kumar , RAO, K., Babu , REDDY, N., Mahhander , REDDY, D., Siva, Prasad
发明人： TYAGI, Om, Dutt , RAY, Purna, Chandra , CHAUHAN, Yogendhra, Kumar , RAO, K., Babu , REDDY, N., Mahhander , REDDY, D., Siva, Prasad
IPC分类号： C07D405/06
CPC分类号： C07D405/06
摘要： The present invention discloses an improved process for producing darifenacin, the process comprising decarboxylating (2S,4R)-4-hydroxy-2-pyrrolidine carboxylic acid followed by in situ tosylation to give l-tosyl-3-(R)-(-)-hydroxypyrrolidine, tosylating the l-tosyl-3-(R)-(-)-hydroxypyrrolidine with methyl-p-toluenesuolphonate to give l-tosyl-3- (S)-(-)-tosyloxy pyrrolidine, reacting l-tosyl-3-(S)-(-)-tosyloxy pyrrolidine with diphenyl acetonitrile in presence of a base to give 3-(S)-(+)-(l-cyano-l,l-diphenylmethyl)-l- tosylpyrrolidine, de-protecting 3-(S)-(+)-(l-cyano-l,l-diphenylmethyl)-l- tosylpyrrolidine in the presence of phenol in acidic medium to give 3-(S)-(+)-(l-cyano- 1,1-diphenylmethyl) pyrrolidine, hydrolyzing 3-(S)-(+)-(l-cyano-l,l-diphenylmethyl) pyrrolidine followed by salt formation to obtain 3-(S)-(+)-(l-carbamoyl-l,l- diphenylmethyl)pyrrolidine.L-(+)-tartrate, condensing 3-(S)-(+)-( 1 -carbamoyl- 1,1- diphenylmethyl)pyrrolidine-L(+)-tartrate with 5-(2-bromoethyl)-2,3-dihydrobenzofuran employing a base in a solvent to give darifenacin.
摘要翻译：本发明公开了一种改进的达赖芬那克的制备方法，该方法包括使（2S，4R）-4-羟基-2-吡咯烷羧酸脱羧，然后进行原位甲苯磺酰化，得到1-甲苯磺酰基-3-（R） - （ - ）（R） - （ - ） - 羟基吡咯烷与甲基对甲苯磺酸酯反应，得到1-甲苯磺酰基-3-（S） - （ - ） - 甲氧基吡咯烷，使1-甲苯磺酰基-3- 在3-（S） - （+） - （1-氰基-1,1-二苯基甲基）-1-甲苯磺酰基吡咯烷存在下，将3-（S） - （ - ） - 甲氧基吡咯烷与二苯基乙腈反应，在酸性介质中在苯酚存在下保护3-（S） - （+） - （1-氰基-1,1-二苯基甲基）-1-甲苯磺酰基吡咯烷，得到3-（S） - （+） - （1-氰基 -1,1-二苯基甲基）吡咯烷，水解3-（S） - （+） - （1-氰基-1,1-二苯基甲基）吡咯烷，接着形成盐，得到3-（S） - （+） - - （+） - 酒石酸盐，将3-（S） - （+） - （1-氨基甲酰基-1,1-二苯基甲基）吡咯烷-L（+） - 酒石酸盐与 5-（2-溴乙基）-2,3--D 使用在溶剂中的碱的二氢苯并呋喃来给予达瑞那新。

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