SYNTHESIS OF HETEROARYL ACETAMIDES FROM REACTION MIXTURES HAVING REDUCED WATER CONTENT

摘要

An improved process for the preparation of a heteroaryl acetamide from a heteroaryl a-hydroxyacetamide is provided. The process comprises directly hydrogenating the heteroaryl a-hydroxyacetamide in the presence of a strong acid, a halide and a catalyst wherein the molar ratio of the starting heteroaryl ­ a-hydroxyacetamide to water at the initiation of hydrogenolysis is at least about 2:1. In one embodiment, the heteroaryl acetamide is zolpidem and the heteroaryl ­ a-hydroxyacetamide is a-hydroxyzolpidem. Formulae (1) and (1A).