Synthesis of deuterated S-217622 (Ensitrelvir) with antiviral activity against coronaviruses including SARS-CoV-2

Yang, Yujian; Cao, Liu; Yan, Ming; Zhou, Jun; Yang, Shibin; Xu, Tingting; Huang, Si-Yao; Li, Kun; Zhou, Qifan; Li, Guanguan; Zhu, Yujun; Feng, Cong; Zhang, Hongmin; Guo, Deyin; Li, Yingjun; Zhang, Xumu

doi:10.1016/j.antiviral.2023.105586

Cited by 3 publications

(1 citation statement)

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“…When trifluorobenzoic acid 17 as raw material was treated with LiAlH 4 in tetrahydrofuran as the solvent, the benzyl alcohol product 18 was obtained in >80.0% yield . Because this reaction is so violent, the temperature has to be kept at 0 °C or controlled by dropwise addition. , A similar high yield was obtained using the reagent NaBH 4 or KBH 4 in alcohol at 0 °C, when aldehyde 19 was used as starting material . After the key trifluorobenzyl alcohol was obtained, sequential bromination using HBr or PBr 3 gave good yield. ,, …”

Section: Synthesis Of Key Building Blocks For Ensitrelvirmentioning

confidence: 91%

Comprehensive Review on the Synthetic Strategies toward Anti-SARS-CoV-2 Drug Ensitrelvir

Liu,

Wu,

Yang

et al. 2024

Org. Process Res. Dev.

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The outbreak and rapid spread of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) have led to one of the most serious public health crises since the beginning of the 21st century. An oral anti-SARS-CoV-2 drug ensitrelvir was developed with satisfactory antiviral effect and was synthesized via different strategies. This Review summarizes the advantages and disadvantages of the currently reported synthetic strategies for ensitrelvir along with three related key building blocks derivatives from the view of procedure, yield, impurities, safety, and environment. This will provide a novel perspective for further process development and drug discovery.

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