Total Synthesis of Carolacton and Demethylcarolactons with Potent Antiviral Activity
Haoyu Zhang,
Bingsong Li,
Hongzhi Yang
et al.
Abstract:Carolacton, a naturally occurring MTHFD1 inhibitor, exhibits potent inhibitory activity against various RNA viruses including SARS-CoV-2. Herein, we present a concise total synthesis of carolacton, featuring the Krische allylation, Marshall coupling, NHK coupling, and RCM reaction as key elements. Additionally, we have synthesized three simplified carolacton analogues, one of which, namely, 14-demethyl-carolacton, exhibited notable antiviral activity. The present work paves the way for further exploration of t… Show more
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