Evolving to an Ideal Synthesis of Molnupiravir, an Investigational Treatment for COVID-19
ChemRxiv(2020)
摘要
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.
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