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

Fier, P. S.; Xu, Y. J.; Poirier, M.; Brito, G.; Zheng, M.; Bade, R.; Sirota, E.; Stone, K.; Tan, L. S.; Humphrey, G. R.; Chang, D.; Bothe, J.; Zhang, Y. Q.; Bernardoni, F.; Castro, S.; Zompa, M. A.; Taylor, J.; Sirk, K. M.; Diaz-Santana, A.; Diribe, I.; Emerson, K. M.; Krishnamurthi, B.; Zhao, R.; Ward, M.; Xiao, C. Q.; Ouyand, H. G.; Zhan, J. F.; Morris, W. J.

Fier, P. S.; Xu, Y. J.; Poirier, M.; Brito, G.; Zheng, M.; Bade, R.; Sirota, E.; Stone, K.; Tan, L. S.; Humphrey, G. R.; Chang, D.; Bothe, J.; Zhang, Y. Q.; Bernardoni, F.; Castro, S.; Zompa, M. A.; Taylor, J.; Sirk, K. M.; Diaz-Santana, A.; Diribe, I.; Emerson, K. M.; Krishnamurthi, B.; Zhao, R.; Ward, M.; Xiao, C. Q.; Ouyand, H. G.; Zhan, J. F.; Morris, W. J..

Organic Process Research & Development ; : 10, 2021.

Article in English | Web of Science | ID: covidwho-1586054

ABSTRACT

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.

Keywords

molnupiravir; covid-19; antiviral; crystallization; derivatives; Chemistry

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Full text: Available Collection: Databases of international organizations Database: Web of Science Language: English Journal: Organic Process Research & Development Year: 2021 Document Type: Article

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