Buchwald reaction as the key step for the synthesis of metabolically more stable analogs of amodiaquine

…, G Hochart, PE Larchanché, P Melnyk

Index: Le Fur, Nicolas; Hochart, Guillaume; Larchanche, Paul-Emmanuel; Melnyk, Patricia European Journal of Medicinal Chemistry, 2011 , vol. 46, # 7 p. 3052 - 3057

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Abstract

Abstract Amodiaquine is one of the most active anti-malarial 4-aminoquinoline but its metabolization is believed to generate hepatotoxic derivatives. Previously, we described new analogs of amodiaquine and amopyroquine, in which hydroxyl group was replaced by various amino groups and identified highly potent compounds with lower toxicity. We describe here the synthesis of new analogs that have been modified on their 4′-and 5′- ...