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

Autor: Jonathan Vroom, Deeptak Verma, Pan W, William J. Morris, Tamas Benkovics, John A. McIntosh, Hao Yang, Tetsuji Itoh, Ho H, Knight A, Hurtak J, Neil A. Strotman, Grant S. Murphy, Peter E. Maligres, Kong J, Patrick S. Fier, Kevin M. Maloney, Steven M. Silverman, Mark A. Huffman
Rok vydání: 2020
Předmět:
Popis: 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.
Databáze: OpenAIRE