Optimized and convergent synthesis of potent anti-malarial aminoquinoline compounds: easy access to analogs

Abstract

Amodiaquine is one of the most active antimalarial 4-aminoquinoline. Previously we have described new analogs of amodiaquine and amopyroquine, in which the hydroxyl group was replaced by various amino groups and identifi ed highly potent compounds. Here we describe a more effi cient synthesis of this family of compounds allowing the rapid and convergent access of new analogs bearing a piperazine or a morpholine ring at the 4 ′ -position and diverse heterocyclic amino side chains.