posted on 2022-07-08, 00:05authored byChao 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.