公开(公告)号：US09403770B2

公开(公告)日：2016-08-02

申请号：US12374539

申请日：2007-07-25

申请人： Giorgio Bertolini ,  Maurizio Gallina ,  Giuseppe Motta ,  Domenico Vergani

发明人： Giorgio Bertolini ,  Maurizio Gallina ,  Giuseppe Motta ,  Domenico Vergani

IPC分类号： C07D211/22

CPC分类号： C07D211/22

摘要： A process for preparing fexofenadine is described, which provides for the hydrolysis of 4-[4-[4-(hydroxydiphenylmethyl)-1-piperidyl]-1-oxobutyl]-α,α-dimethylbenzeneacetic acid-alkyl ester, in a mixture of water and optionally an organic solvent, in the presence of a base; the carboxylate salt of 4-[4-[4-(hydroxydiphenylmethyl)-1-piperidyl]-1-oxobutyl]-α,α-dimethylbenzeneacetic acid is thus obtained, which is then directly reduced as carboxylate in a basic environment with hydrogen in the presence of a suitable hydrogenation catalyst to give the carboxylate of fexofenadine, which is precipitated by neutralization of the solution.

摘要翻译： 描述了制备非索非那定的方法，其提供4- [4- [4-（羟基二苯基甲基）-1-哌啶基] -1-氧代丁基]-α，α-二甲基苯乙酸 - 烷基酯在水溶液 水和任选的有机溶剂，在碱的存在下; 由此得到4- [4- [4-（羟基二苯基甲基）-1-哌啶基] -1-氧代丁基]-α，α-二甲基苯乙酸的羧酸盐，然后在碱性环境中用氢气将其直接还原为羧酸盐 存在合适的氢化催化剂以得到通过溶液中和而沉淀的非索非那定的羧酸盐。

公开(公告)号：US20090209754A1

公开(公告)日：2009-08-20

申请号：US12319292

申请日：2009-01-05

申请人： Peter Lindsay MacDonald ,  Pierluigi Rossetto ,  Maurizio Gallina

发明人： Peter Lindsay MacDonald ,  Pierluigi Rossetto ,  Maurizio Gallina

IPC分类号： C07H19/06

CPC分类号： C07H19/06 ,  C07D405/04 ,  C07H1/00

摘要： The present application relates to an improved process for the preparation of capecitabine.

摘要翻译： 本申请涉及用于制备卡培他滨的改进方法。

公开(公告)号：US20110190504A1

公开(公告)日：2011-08-04

申请号：US12374539

申请日：2007-07-25

申请人： Giorgio Bertolini ,  Maurizio Gallina ,  Giuseppe Motta ,  Domenico Vergani

发明人： Giorgio Bertolini ,  Maurizio Gallina ,  Giuseppe Motta ,  Domenico Vergani

IPC分类号： C07D211/34

CPC分类号： C07D211/22

摘要： A process for preparing fexofenadine is described, which provides for the hydrolysis of 4-[4-[4-(hydroxydiphenylmethyl)-1-piperidyl]-1-oxobutyl]-α,α-dimethylbenzeneacetic acid-alkyl ester, in a mixture of water and optionally an organic solvent, in the presence of a base; the carboxylate salt of 4-[4-[4-(hydroxydiphenylmethyl)-1-piperidyl]-1-oxobutyl]-α,α-dimethylbenzeneacetic acid is thus obtained, which is then directly reduced as carboxylate in a basic environment with hydrogen in the presence of a suitable hydrogenation catalyst to give the carboxylate of fexofenadine, which is precipitated by neutralisation of the solution.

摘要翻译： 描述了制备非索非那定的方法，其提供4- [4- [4-（羟基二苯基甲基）-1-哌啶基] -1-氧代丁基]-α，α-二甲基苯乙酸 - 烷基酯在水溶液 水和任选的有机溶剂，在碱的存在下; 由此得到4- [4- [4-（羟基二苯基甲基）-1-哌啶基] -1-氧代丁基]-α，α-二甲基苯乙酸的羧酸盐，然后在碱性环境中用氢气将其直接还原为羧酸盐 存在合适的氢化催化剂以得到通过溶液中和而沉淀的非索非那定的羧酸盐。