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Tricyclic Aza-Andrographolide Derivatives from Late-Stage Hydroamination and Their Anti-human Coronavirus (Anti-HCoV) Activity

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posted on 2022-07-08, 00:05 authored by Chao Che, Ding Jiang, Jiayin Zhang, Qi Xing, Ting Li, Yi Zhao, Liangyu Guan, Huangcan Chen, Dehu Xiang, Man Di, Zhendong Zhu
A late-stage functionalization (LSF) of the natural product andrographolide for the efficient assembly of a range of structurally interesting and diverse tricyclic-aza derivatives was developed. The key to the diversification is a photo-catalyzed intramolecular hydroamination reaction, and acridinium derivatives were demonstrated to be the optimal catalysts. Additionally, the synthesized tricyclic aza-andrographolide derivatives were found to inhibit human coronavirus with high potency.

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