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

Eric YuHari P R MangunuruNakul S TelangCaleb J KongJenson VergheseStanley E Gilliland IiiSaeed AhmadRaymond N DomineyB Frank Gupton
Published in: Beilstein journal of organic chemistry (2018)
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.
Keyphrases
  • highly efficient
  • plasmodium falciparum
  • emergency department
  • anaerobic digestion
  • high resolution
  • combination therapy