阿莫地喹
过程(计算)
化学
药理学
计算机科学
疟疾
医学
氯喹
操作系统
免疫学
作者
Mukut Gohain,Modibo S. Malefo,Phaladi Kunyane,Chantal Scholtz,Sangeeta Baruah,Andile Zitha,Gerrit van der Klashorst,Hannes Malan
标识
DOI:10.1021/acs.oprd.3c00205
摘要
A robust process 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, substitution with 4,7-dichloroquinoline (4,7-DCQ, 5), and rehydration. Additionally, a cost-competitive process for the production of 4,7-DCQ (5) is also reported wherein 4,7-DCQ (5) was prepared in four steps from meta-chloroaniline (7). 4-Acetamido-2-(diethylaminomethyl)phenol (14), 4,7-DCQ (5), and ADQ (3) were obtained in yields of 92, 89, and 90%, respectively. Costing and process mass intensities of 4,7-DCQ and ADQ are also reported.
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