Patent ID: 7498439
Filing Date: 2009-03-03
Classification: C07D

Abstract:
1. A process for the preparation of a heteroaryl acetamide from a heteroaryl α-hydroxyacetamide, the process comprising directly hydrogenating a heteroaryl α-hydroxyacetamide in the presence of hydrogen gas in a reaction mixture comprising a solvent system, the heteroaryl α-hydroxyacetamide, at least one strong acid, a halide and a precious metal catalyst, wherein the reaction mixture has a molar ratio of the starting heteroaryl α-hydroxyacetamide to water at the initiation of hydrogenolysis of at least about 2:1, the heteroaryl α-hydroxyacetamide corresponding to Formula 1 and the heteroaryl acetamide product corresponding to Formula 1A: wherein Z is O, NR X R R R R R R n is 0 or 1; each Y is independently hydrogen, halogen or C when Z is CR