Patent ID: 8962851
Filing Date: 2015-02-24
Classification: C07D

Abstract:
1. A one-pot process for preparing 2-[(pyridinyl)methyl]sulfinyl-benzimidazole derivative of Formula (II′) or a pharmaceutically acceptable salt of Formula (I′), hydrate or a solvate thereof, wherein M is alkali or alkaline earth metal salts; R R R (a) reacting 2-chloromethyl-substituted pyridine of Formula (V′) or a salt thereof with 2-mercapto-5-substituted benzimidazole of Formula (IV′) in one or more suitable organic solvents, optionally in the presence of a base to obtain prochiral sulfide of Formula (III′); (b) asymmetrically oxidizing prochiral sulfide of Formula (III′) in-situ with an oxidizing agent in one or more organic solvents in the presence of a chiral transition metal complex, and optionally in the presence of a base to obtain optically active enantiomer or an enantiomerically enriched form of a compound of Formula (II′); wherein R (c) optionally, converting the optically active enantiomer or an enantiomerically enriched form of the compound of Formula (II′) to a pharmaceutically acceptable salt thereof of Formula (I′), hydrate or solvate thereof; and (d) obtaining 2-[(pyridinyl)methyl]sulfinyl-benzimidazole derivative of Formula (II′) or a pharmaceutically acceptable salt of Formula (I′), hydrate or a solvate thereof.