lmproved process of dexrabeprazole sodium
10.11665/j.issn.1000-5048.20180306
- VernacularTitle:右旋雷贝拉唑钠的制备工艺改进
- Author:
Chunlai ZHANG
1
;
Hongjun LUO
;
Qi JIANG
;
Guoxian LI
;
Guoqing GU
;
Jie ZHANG
Author Information
1. 扬子江药业集团有限公司
- Keywords:
dexrabeprazole;
asymmetric oxidation;
synthetic process
- From:
Journal of China Pharmaceutical University
2018;49(3):291-294
- CountryChina
- Language:Chinese
-
Abstract:
The aim of the work is to improve the synthetic process of dexrabeprazole sodium,enhance quality and yield of the product,simplify synthetic steps,and offer a stable and feasible process. Starting from 2-[[[4-(3-methoxypropoxy)-3-methylpyridine-2-yl]methyl]thio]-1 H-benzimidazole,dexrabeprazole was produced by asym-metric oxidation reaction with oxidant cumene hydroperoxide in the presence of chiral catalyst tetraisopropyl titan-ate and L-(+)-tartaric acid diethyl ester. Dexrabeprazole sodium was obtained by the reaction of purified dexrabeprazole with sodium hydroxide in a total yield of 79%with an HPLC purity of ＞99. 5%. The structure of dexrabeprazole sodium was confirmed by NMR,IR,elemental analysis and LC-MS. The improved process of dexrabeprazole sodium possesses simple operations,good yield and high purity,which is feasible for industrializa-tion.
