lmproved process of dexrabeprazole sodium / 中国药科大学学报

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.