PREPARATION METHOD FOR NEBIVOLOL INTERMEDIATE AND PREPARATION METHOD FOR NEBIVOLOL

WIPO Patent Application WO/2016/115962

A1

Provided is a preparation method for a Nebivolol intermediate of compounds of formula V, which comprises one of the methods as follows: (1) a RS/RR-IV compound and a compound of formula S-I are subjected to a coupling and docking reaction to obtain a material containing a compound of formula RS#S-V and a compound of formula RR#S-V, and the compounds of formula V in two configurations are separated; and (2) a SR/SS-IV compound and a compound of formula R-I are subjected to a coupling and docking reaction to obtain a material containing a compound of formula SR#R-V and a compound of formula SS#R-V, and the compounds of formula V in two configurations are separated. Further, also provided is a method for preparing Nebivolol or a pharmaceutically acceptable salt thereof from the above-mentioned compounds of formula V. The methods in the present invention have the characteristics of simple and convenient operation, mild reaction conditions, good atomic economy, high yield, low cost and the like, and are suitable for industrial production.

LI HONGMING (CN)
CHU CHANGHU (CN)
JI DUMING (CN)
MIAO CUNQIAN (CN)
BI JIANHAO (CN)
YANG GUOSHENG (CN)

PCT/CN2015/099448

July 28, 2016

December 29, 2015

Click for automatic bibliography generation  

ZHEJIANG HISOAR PHARMACEUTICAL CO LTD (CN)
SHANGHAI HISOAR PHARMACEUTICAL TECHNOLOGY & DEV CO LTD (CN)

C07D311/58

CN104610215A	2015-05-13
EP1803716A1	2007-07-04
CN102164906A	2011-08-24
US20130005001A1	2013-01-03
CN102816141A	2012-12-12

BOSS & YOUNG PATENT AND TRADEMARK LAW OFFICE (CN)
北京邦信阳专利商标代理有限公司 (CN)

View/Download PDF      PDF Help

Previous Patent: ENHANCED POSITIONING METHOD FOR MOVING TARGET IN MINE SHAFT BASED ON WITNESS NODES UNDER INTERNET OF...

Next Patent: DEDICATED FERTILIZER FOR INCREASING ORIGINAL ECOLOGICAL AROMA OF SICHUAN PEPPER AND APPLICATIONS