Development of a Robust Manufacturing Route for Molnupiravir, an Antiviral for the Treatment of COVID-19

  • Org Process Res Dev. 2021 Dec 17;25(12):2806-2815. doi: 10.1021/acs.oprd.1c00400.
Patrick S Fier  1 ,  Yingju Xu  1 ,  Marc Poirier  1 ,  Gilmar Brito  1 ,  Michelle Zheng  1 ,  Rachel Bade  1 ,  Eric Sirota  1 ,  Kevin Stone  1 ,  Lushi Tan  1 ,  Guy R Humphrey  1 ,  Darryl Chang  1 ,  Jameson Bothe  1 ,  Yongqian Zhang  1 ,  Frank Bernardoni  1 ,  Steve Castro  1 ,  Michael A Zompa  1 ,  Jerry Taylor  1 ,  Kevin M Sirk  1 ,  Anthony Diaz-Santana  1 ,  Ike Diribe  1 ,  Khateeta M Emerson  1 ,  Bharath Krishnamurthi  1 ,  Ralph Zhao  1 ,  Michael Ward  1 ,  Chengqian Xiao  2 ,  Honggui Ouyand  2 ,  Jianfeng Zhan  2 ,  William J Morris  1
Affiliations
  • 1. Department of Process Research and Development, Merck & Co., Inc., Rahway, New Jersey 07065, United States.
  • 2. WuXi AppTec Co., Ltd., WaiGaoQiao Free Trade Zone, Shanghai 200131, China.
PMID: 35095257 DOI: 10.1021/acs.oprd.1c00400
Abstract

Herein is described the development of a large-scale manufacturing process for molnupiravir, an orally dosed Antiviral that was recently demonstrated to be efficacious for the treatment of patients with COVID-19. The yield, robustness, and efficiency of each of the five steps were improved, ultimately culminating in a 1.6-fold improvement in overall yield and a dramatic increase in the overall throughput compared to the baseline process.

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