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 alpha-hydroxyacetamide is provided. The process comprises directly hydrogenating the heteroaryl alpha-hydroxyacetamide in the presence of a strong acid, a halide and a catalyst wherein the molar ratio of the starting heteroaryl alpha-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 alpha-hydroxyacetamide is alpha-hydroxyzolpidem.