Mukut Gohain, Modibo S. Malefo, Phaladi Kunyane
Dec 18, 2023
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Journal
Organic Process Research & Development
Abstract
A robust process technology for the manufacture of the active pharmaceutical ingredient (API) amodiaquine dihydrochloride dihydrate (ADQ, 3 ), an important antimalarial, is reported. The process consists of a three-step synthetic route that involves a Mannich reaction, condensation with 4,7-dichloroquinoline (DCQ, 5 ) and rehydration. Additionally, a cost-competitive process for the production of DCQ ( 5 ) is also reported wherein DCQ ( 5 ) was prepared in four steps from meta -chloroaniline ( 7 ). 4-Amido-2-(diethylaminomethyl)phenol ( 14 ), DCQ ( 5 ), and ADQ ( 3 ) were obtained in yields of 92, 89 and 90% respectively.