Diastereoselective synthesis hydroxyethylene dipeptide isosteres

摘要

A process for the synthesis of hydroxyethylene dipeptide isosteres from alpha -N,N-di(protected)amino(alkyl or substituted alkyl) methyl ketones that can be efficiently carried out on an industrial scale. The process proceeds with excellent diastereoselectivity and chemical efficiency, and can be used to prepare a wide variety of hydroxyethylene dipeptide isosteres for a variety of uses, including as HIV-1 protease inhibitors and renin inhibitors.