Abstract
Herein,
we reported a convenient and cost efficient one-pot synthesis of molnupiravir
from cytidine. This method utilized N,N-dimethylformamide dimethyl acetal (DMF-DMA)
as an extraordinary protecting agent to achieve site specific esterification at 5’-hydroxyl group of the nucleoside easily, and afforded this promising drug
candidate (purity up to 99%, HPLC a/a) in 70% overall yield without
chromatography purification, which is superior to the existing methods in
aspect of the yield, the cost and the operation, and shows great potential
value for commercial production. Furthermore, this excellent protecting agent
was also successfully used in the synthesis of remdesivr from its parent
nucleoside with a high total yield (76%).
Content

Supplementary material

supporting information