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High-yielding continuous-flow synthesis of antimalarial drug hydroxychloroquine.

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.

SUBMITTER: Yu E

PROVIDER: S-EPMC5852550 | biostudies-other | 2018

REPOSITORIES: biostudies-other

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High-yielding continuous-flow synthesis of antimalarial drug hydroxychloroquine.

Yu Eric E Mangunuru Hari P R HPR Telang Nakul S NS Kong Caleb J CJ Verghese Jenson J Gilliland Iii Stanley E SE Ahmad Saeed S Dominey Raymond N RN Gupton B Frank BF

Beilstein journal of organic chemistry 20180308

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 ...[more]

PMID: 29623120

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