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Beilstein J Org Chem. 2018 Mar 8;14:583-592. doi: 10.3762/bjoc.14.45. eCollection 2018.

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

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Department of Chemistry and Department of Chemical and Life Science Engineering, Virginia Commonwealth University, 601 W. Main St., Richmond, VA 23220, USA.
Contributed equally


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.


API manufacturing; antimalarial; flow chemistry; hydrogenation; hydroiodic acid; hydroxychloroquine

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