公开(公告)号：EP2801567A1

公开(公告)日：2014-11-12

申请号：EP12862614.0

申请日：2012-07-27

申请人： Zhejiang Jiuzhou Pharmaceutical Co., Ltd.

发明人： ZHANG, Bin ,  HU, Xiaowei ,  YAN, Pucha ,  ZHANG, Xianyi ,  GAO, Hongjun ,  LI, Yuanqiang ,  CHE, Daqing

IPC分类号： C07D209/08 ,  C07D209/04 ,  C07D209/02 ,  C07F7/18 ,  C07F7/02 ,  C07F7/00

CPC分类号： C07D209/08 ,  C07F7/00 ,  C07F7/02 ,  C07F7/18 ,  C07F9/65397 ,  Y02P20/55

摘要： Disclosed are a silodosin intermediate and a preparation method thereof. The silodosin intermediate has the structure shown by the formula (A). X is hydrogen or bromide and R 1 is hydrogen. The formyl group may be a group having the structure shown by the formula I. R 7 is an carboxyl-protecting group, and R 2 is 3-hydroxypropyl or a group having the structure shown by the formula II. W is a hydroxyl-protecting group. A compound of the formula (A) according to the present invention may further be used for preparing a compound having the structure shown by the formula (D). By means of the intermediate and the preparation method therefor provided by the present invention, high-purity optically pure silodosin can be obtained, and the optical purity is above 99%.

摘要翻译： 公开了一种西洛多辛中间体及其制备方法。 西洛多辛中间体具有式（A）所示的结构。 X是氢或溴，R1是氢。 甲酰基可以是具有式I所示结构的基团。R 7是羧基保护基，R 2是3-羟基丙基或具有式II所示结构的基团。 W是羟基保护基。 根据本发明的式（A）化合物还可以用于制备具有式（D）所示结构的化合物。 通过本发明提供的中间体及其制备方法，可以得到高纯度的光学纯的西洛多辛，光学纯度在99％以上。