Convenient Procedure for Synthesis of N-Protected beta-Aminomalonates and beta-Amino Acids From alpha-Amidosulfones

摘要

A synthesis of N-protected beta-aminomalonates starting from alpha-amidosulfones under very mild and simple reaction conditions is described.Treatment of the sulfones with malonate esters in the presence of 2.5 equivalents of potassium carbonate affords the desired products in good yield.A variety of N-Z and N-Boc protected aliphatic and aromatic alpha-aminosulfones and malonate esters have been successfully used as starting materials.Hydrolysis with concomitant decarboxylation of the N-protected beta-aminomalonates provides a convenient access to racemic beta-amino acids.