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Evolving to an Ideal Synthesis of Molnupiravir, an Investigational Treatment for COVID-19

preprint
submitted on 21.12.2020, 19:45 and posted on 23.12.2020, 04:57 by Tamas Benkovics, John McIntosh, Steven Silverman, Jongrock Kong, Peter Maligres, Tetsuji Itoh, Hao Yang, Mark Huffman, Deeptak Verma, Weilan Pan, Hsing-I Ho, Jonathan Vroom, Anders Knight, Jessica Hurtak, William Morris, Neil Strotman, Grant Murphy, Kevin Maloney, Patrick Fier

Molnupiravir (MK-4482) is an investigational direct-acting antiviral agent that is under development for the treatment of COVID-19. Given the potential high demand for this compound, it was critical to develop a sustainable and efficient synthesis from commodity raw materials. The three-step route that we report here embodies the shortest possible synthesis to molnupiravir, and was enabled through the invention of a novel biocatalytic cascade and final condensation step. Each step occurs in over 95% yield and only utilizes widely available commodity reagents and simple operations. Compared to the initial route, the new route is 70% shorter, and approximately seven-fold higher in overall yield.

History

Email Address of Submitting Author

patrick.fier@merck.com

Institution

Merck & Co., Inc

Country

United States of America

ORCID For Submitting Author

0000-0002-6102-815X

Declaration of Conflict of Interest

N/A

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