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 identified highly potent compounds. Here we describe a more efficient 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.