Synthesis of aliskiren

Abstract

This paper describes a practical process for the preparation of aliskiren.Chiral building blocks 1 and 2 were prepared by chemical resolution,and a following five-step convergent synthesis led to aliskiren with an overall yield of 15.6%.The intermediates and the target compound were characterized by melting points,NMR and MS.The convergent synthetic process of aliskiren highlights reasonable yields,ease of operation,high stereoselectivity as well as only one chromatographic purification,and thus should be amenable to large-scale production.