Synthesis of heteroaryl acetamides from reaction mixtures...

Details Synthesis of heteroaryl acetamides from reaction mixtures... Synthesis of heteroaryl acetamides from reaction mixtures...

C - Chemistry, Metallurgy

07

D

C07D 471/04 (2006.01)

Patent

CA 2571491

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. Formulae (1) and (1A).

Procédé amélioré pour la préparation d~un acétamide hétéroaryle à partir d~un .alpha.-hydroxyacétamide hétéroaryle. Le procédé comprend l~hydrogénation directe de l~.alpha.-hydroxyacétamide hétéroaryle en présence d~un acide fort, un halogénure et un catalyseur où le rapport molaire entre l~.alpha.-hydroxyacétamide hétéroaryle de départ et l~eau au début de l~hydrogénolyse est d~au moins 2:1. Selon un mode de réalisation, l~acétamide hétéroaryle est le zolpidem et l~.alpha.-hydroxyacétamide hétéroaryle est l~.alpha.-hydroxyzolpidem. Formules (1) and (1A).

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