PROCESS FOR PRODUCING 3-AMINO-2-OXO-1-HALOGENOPROPANE DERIVATIVES

摘要

3-Amino-2-oxo-1-halogenopropane derivatives are prepared by reacting a protected amino acid with an alkali metal enolate of an alkyl acetate with a halogenating agent for halogenation of the 2-position, or by reacting a protected amino acid with an alkali metal enolate of an alkyl halogenoacetate, to form a 4-amino-3- oxo-2-halogenobutanoic acid ester derivative which is then hydrolyzed and decarboxylated. The 3-amino-2-oxo-1- halogenopropane derivatives obtained in accordance with the invention can easily be converted to 3-amino-1,2- epoxypropanes that are important as intermediates for pharmaceutical preparations including HIV protease inhibitors and certain enzyme inhibitors.