-
公开(公告)号:US20100249438A1
公开(公告)日:2010-09-30
申请号:US12749569
申请日:2010-03-30
申请人: Vijaya Bhaskar Bolugoddu , Chandrasekhar Ravi Ram Elati , Sasi Kala Venkata Annapurna Cheemalapati , Rajagopal Penumandla , Arulnathan Prabakar Christy , Lakshmi Vara Prasad Sree Naga Venkata Vakamudi
发明人: Vijaya Bhaskar Bolugoddu , Chandrasekhar Ravi Ram Elati , Sasi Kala Venkata Annapurna Cheemalapati , Rajagopal Penumandla , Arulnathan Prabakar Christy , Lakshmi Vara Prasad Sree Naga Venkata Vakamudi
IPC分类号: C07D307/79
CPC分类号: C07D307/87
摘要: A substantially pure (S)-4-[4-(dimethylamino)-1-(4′-fluorophenyl)-1-hydroxybutyl]-3-(hydroxymethyl)benzonitrile intermediate for preparing escitalopram is prepared by:a) combining racemic (±)-4-[4-(dimethylamino)-1-(4′-fluorophenyl)-1-hydroxybutyl]-3-(hydroxymethyl)benzonitrile with (−)-di-p-toluoyltartaric acid, in a solvent;b) separating a solid phase comprising a salt of (−)-di-p-toluyltartaric acid with (R)-4-[4-(dimethylamino)-1-(4′-fluorophenyl)-1-hydroxybutyl]-3-(hydroxymethyl)benzonitrile enantiomer, and a liquid phase comprising a salt of (−)-di-p-toluoyltartaric acid with (S)-4-[4-(dimethylamino)-1-(4′-fluorophenyl)-1-hydroxy-butyl]-3-(hydroxymethyl)benzonitrile enantiomer;c) reacting the liquid phase with a base and isolating enantiomerically enriched (S)-4-[4-(dimethylamino)-1-(4′-fluorophenyl)-1-hydroxybutyl]-3-(hydroxymethyl)benzonitrile enantiomer;d) combining enantiomerically enriched (S)-enantiomer obtained in c) with (+)-di-p-toluoyltartaric acid, in a solvent; ande) reacting a precipitate from d) with a base.
摘要翻译: 制备用于制备依他普仑的基本上纯的(S)-4- [4-(二甲基氨基)-1-(4'-氟苯基)-1-羟基丁基] -3-(羟甲基)苄腈中间体是通过以下步骤制备的:a)将外消旋 )-4- [4-(二甲基氨基)-1-(4'-氟苯基)-1-羟基丁基] -3-(羟甲基)苄腈与( - ) - 二 - 对甲苯甲酰酒石酸在溶剂中; b)将( - ) - 二 - 对 - 甲苯基酒石酸盐与(R)-4- [4-(二甲基氨基)-1-(4'-氟苯基)-1-羟基丁基] -3- (羟甲基)苄腈对映异构体,以及包含( - ) - 二对甲苯甲酰酒石酸与(S)-4- [4-(二甲基氨基)-1-(4'-氟苯基)-1-羟基 - 丁基] -3-(羟甲基)苄腈对映异构体; c)使液相与碱反应并分离对映异构体富集的(S)-4- [4-(二甲基氨基)-1-(4'-氟苯基)-1-羟基丁基] -3-(羟甲基)苄腈对映异构体; d)将c)中得到的对映异构体富集的(S) - 对映体与(+) - 对 - 甲苯甲酰酒石酸在溶剂中组合; 和e)使来自d)的沉淀物与碱反应。
-
公开(公告)号:US20090048336A1
公开(公告)日:2009-02-19
申请号:US12193201
申请日:2008-08-18
IPC分类号: A61K31/343 , C07D307/87 , A61P25/24
CPC分类号: C07D307/87
摘要: Escitalopram oxalate powders having definite particle size distribution parameters, processes for preparing the powders, and solid pharmaceutical formulations containing the powders.
摘要翻译: 具有确定的粒度分布参数的草酮草铵盐粉末,制备粉末的方法和含有粉末的固体药物制剂。
-
公开(公告)号:US20080214535A1
公开(公告)日:2008-09-04
申请号:US11997203
申请日:2006-07-31
申请人: Vijayavitthal Thippannachar Mathad , Pravinchandra Vankawala Jayantilal , Chandrasekhar Ravi Ram Elati , Subrahmanyeswara Rao Chlamala , Naveen Kumar Kolla , Srinivas Gangula , Srirami Reddy Kikkuru , Srinivasan Neti , Raveendra Reddy Chinta
发明人: Vijayavitthal Thippannachar Mathad , Pravinchandra Vankawala Jayantilal , Chandrasekhar Ravi Ram Elati , Subrahmanyeswara Rao Chlamala , Naveen Kumar Kolla , Srinivas Gangula , Srirami Reddy Kikkuru , Srinivasan Neti , Raveendra Reddy Chinta
IPC分类号: A61K31/5377
CPC分类号: A61K31/496 , A61K9/146 , A61K47/32
摘要: A coprecipitate comprising amorphous aprepitant and a pharmaceutically acceptable carrier is prepared by rapidly removing solvent from a solution containing aprepitant and the carrier.
摘要翻译: 通过从含有阿维地丁和载体的溶液中快速除去溶剂来制备包含无定形阿拉曲珠和药学上可接受的载体的共沉淀物。
-
-