Che Chao, Jiang Ding, Zhang Jiayin, Xing Qi, Li Ting, Zhao Yi, Guan Liangyu, Chen Huangcan, Xiang Dehu, Di Man, Zhu Zhendong
BayRay Innovative Center, Shenzhen Bay Laboratory, Shenzhen 518032, China.
State Key Laboratory of Chemical Oncogenomics, Guangdong Provincial Key Laboratory of Chemical Genomics, Peking University Shenzhen Graduate School, Shenzhen 518055, China.
ACS Omega. 2022 Jul 7;7(28):24824-24837. doi: 10.1021/acsomega.2c02979. eCollection 2022 Jul 19.
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.
已开发出一种用于高效组装一系列结构有趣且多样的三环氮杂衍生物的天然产物穿心莲内酯的后期功能化（LSF）方法。多样化的关键是光催化分子内氢胺化反应，并且吖啶鎓衍生物被证明是最佳催化剂。此外，发现合成的三环氮杂穿心莲内酯衍生物具有高效抑制人冠状病毒的能力。
