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High-yielding continuous-flow synthesis of antimalarial drug hydroxychloroquine

By Yu, E; Mangunuru, HPRTelang, NS; Kong, CJ; Verghese, J; Gilliland, SE; Ahmad, S; Dominey, RN; Gupton, BF

Published on CMKC

Abstract

Numerous synthetic methods for the continuous preparation of fine chemicals and active pharmaceutical ingredients (API's) have been reported in recent years resulting in a dramatic improvement in process efficiencies. Herein we report a highly efficient continuous synthesis of the antimalarial drug hydroxychloroquine (HCQ). Key improvements in the new process include the elimination of protecting groups with an overall yield improvement of 52% over the current commercial process. The continuous process employs a combination of packed bed reactors with continuous stirred tank reactors for the direct conversion of the starting materials to the product. This high-yielding, multigram-scale continuous synthesis provides an opportunity to achieve increase global access to hydroxychloroquine for treatment of malaria.

Journal

Beilstein Journal of Organic Chemistry. Volume 14, 2018, 583-592

DOI

10.3762/bjoc.14.45

Type of publication

Peer-reviewed journal

Affiliations

  • Virginia Commonwealth University

Article Classification

Research Article

Classification Areas

  • API

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