| 发明名称 |
EFFICIENT PROCESS FOR THE PREPARATION OF ESOMEPRAZOLE (S)-BINOL COMPLEX |
| 摘要 |
Object of the present invention is an improved process for the preparation of Esomeprazole (S)-BINOL complex which is a key intermediate for the synthesis of Esomeprazole and salts thereof. |
| 申请公布号 |
US2016244428(A1) |
申请公布日期 |
2016.08.25 |
| 申请号 |
US201514745481 |
申请日期 |
2015.06.22 |
| 申请人 |
F.I.S. - Fabbrica Italiana Sintetici S.p.A. |
发明人 |
STABILE PAOLO;BERTOLAZZI MORENO;FACCIN NICOLA;RASIA DIEGO |
| 分类号 |
C07D401/12;C07C37/00 |
主分类号 |
C07D401/12 |
| 代理机构 |
|
代理人 |
|
| 主权项 |
1. Process for the preparation of Esomeprazole (S)-(−)-BINOL complex of formula (I):comprising the following steps:
A. providing a mixture of the optical isomers of the compound of formula (III):wherein the chiral center is on the sulfur atom, in dichloromethane;
B. adding to the mixture of the step A from 0.8 to 3.0 molar equivalents of (S)-(−)-BINOL; C. adding an ethereal solvent containing from 5 to 10 atoms of carbon; D. stirring; E. isolating Esomeprazole (S)-(−)-BINOL complex of formula (I). |
| 地址 |
Montecchio Maggiore IT |
