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A Convenient and Cost Efficient Route Suitable for “One-Pot” Synthesis of Molnupiravir

preprint
submitted on 12.03.2021, 16:41 and posted on 16.03.2021, 05:23 by Tianwen Hu, Yuanchao Xie, Yin Liu, Haitao Xue, Fuqiang Zhu, Haji A. Aisa, Jingshan Shen
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%).

Funding

National Science & Technology Major Project “Key New Drug Creation and Manufacturing Program”, China

2020 ANSO Collaborative Research Project

History

Email Address of Submitting Author

hutianwen2009@126.com

Institution

Xinjiang Technical Institute of Physics and Chemistry, Chinese Academy of Sciences

Country

China

ORCID For Submitting Author

0000-0003-2997-8232

Declaration of Conflict of Interest

no conflict of interest

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