Synthesis of Two Neurokinin NK1 Receptor Antagonists: (+)-L-733,060 and (-)-L-733,061

Abstract

This review describes synthetic approaches to (+)-L-733,060 and (-)-L-733,061 reported since 1994, focusing on methods allowing the construction and control of the two stereogenic centers.The methods are divided into three groups: (1) resolution of racemates (chemical or enzymatic resolution), (2) diastereoselective reactions using chiral pools or auxiliaries, and (3) enantioselective reactions (aminohydroxylation, epoxidation, deprotonation, allylic amination, aza-Henry reaction, vinylogous aldolization).CONTENTS 3-2.