公开(公告)号：US10723735B2

公开(公告)日：2020-07-28

申请号：US16495275

申请日：2018-03-29

Applicant: Novartis AG

Inventor： Fabrice Gallou ,  Philipp Lustenberger ,  Christian Mathes ,  Qiangbiao Pan ,  Benli Zou

IPC: C07D471/04 ,  B01J23/44 ,  B01J27/128

Abstract: This invention relates to novel processes for synthesizing [1-(4-Methanesulfonyl-2-trifluoromethyl-benzyl)-2-methyl-1H-pyrrolo[2,3-b]pyridin-3-yl]-acetic acid and to intermediates that are used in such processes.

公开(公告)号：US20130096337A1

公开(公告)日：2013-04-18

申请号：US13705884

申请日：2012-12-05

Applicant: Novartis AG

Inventor： Christian Mathes ,  Michael Foulkes ,  Martin Kesselgruber

IPC: C07C269/04 ,  C07C213/02 ,  C07C309/66 ,  C07C37/00

CPC classification number: C07C269/04 ,  C07B2200/07 ,  C07C37/002 ,  C07C213/02 ,  C07C213/08 ,  C07C303/28 ,  C07C303/30 ,  C07C309/66 ,  C07C215/50 ,  C07C39/11

Abstract: A catalytic process for the preparation of optically active compounds and their conversion thereafter to desired drug substances. In particular, the process relates to the preparation of (S)-3-(1-Dimethylamino-ethyl)-phenol using asymmetric catalytic reduction and transfer hydrogenation, thereby providing an improved route to forming drug substances such as rivastigimine and rivastigimine hydrogen tartrate.

Abstract translation: 用于制备光学活性化合物的催化方法及其转化为所需药物。 具体而言，该方法涉及使用不对称催化还原和转移氢化制备（S）-3-（1-二甲基氨基 - 乙基） - 苯酚，从而提供形成药物物质如拉伐斯他明和酒石酸氢铵的改进途径。

公开(公告)号：US20200031824A1

公开(公告)日：2020-01-30

申请号：US16495275

申请日：2018-03-29

Applicant: Novartis AG

Inventor： Fabrice Gallou ,  Philipp Lustenberger ,  Christian Mathes ,  Qiangbiao Pan ,  Benli Zou

IPC: C07D471/04 ,  B01J27/128 ,  B01J23/44

Abstract: This invention relates to novel processes for synthesizing [1-(4-Methanesulfonyl-2-trifluoromethyl-benzyl)-2-methyl-1H-pyrrolo[2,3-b]pyridin-3-yl]-acetic acid and to intermediates that are used in such processes.

公开(公告)号：US08637713B2

公开(公告)日：2014-01-28

申请号：US13705884

申请日：2012-12-05

Applicant: Novartis AG

Inventor： Christian Mathes ,  Michael Foulkes ,  Martin Kesselgruber

IPC: C07C37/00 ,  C07C213/02 ,  C07C269/00 ,  C07C309/65 ,  A61K31/095

CPC classification number: C07C269/04 ,  C07B2200/07 ,  C07C37/002 ,  C07C213/02 ,  C07C213/08 ,  C07C303/28 ,  C07C303/30 ,  C07C309/66 ,  C07C215/50 ,  C07C39/11

Abstract: A catalytic process for the preparation of optically active compounds and their conversion thereafter to desired drug substances. In particular, the process relates to the preparation of (S)-3-(1-Dimethylamino-ethyl)-phenol using asymmetric catalytic reduction and transfer hydrogenation, thereby providing an improved route to forming drug substances such as rivastigimine and rivastigimine hydrogen tartrate.

Abstract translation: 用于制备光学活性化合物的催化方法及其转化为所需药物。 具体而言，该方法涉及使用不对称催化还原和转移氢化制备（S）-3-（1-二甲基氨基 - 乙基） - 苯酚，从而提供形成药物物质如拉伐斯他明和酒石酸氢铵的改进途径。