Bio-Inspired Fragmentations: Rapid Assembly of Indolones, 2-Quinolinones, and (−)-Goniomitine
Haokun Li
School of Pharmaceutical Sciences, Tsinghua University, Beijing, 100084 China
These authors contributed equally to this work.
Search for more papers by this authorPeng Cheng
Collaborative Innovation Center for Biotherapy, West China Medical School, Sichuan University, Chengdu, 610041 China
These authors contributed equally to this work.
Search for more papers by this authorLong Jiang
School of Pharmaceutical Sciences, Tsinghua University, Beijing, 100084 China
Search for more papers by this authorProf. Dr. Jin-Liang Yang
Collaborative Innovation Center for Biotherapy, West China Medical School, Sichuan University, Chengdu, 610041 China
Search for more papers by this authorCorresponding Author
Prof. Dr. Liansuo Zu
School of Pharmaceutical Sciences, Tsinghua University, Beijing, 100084 China
Collaborative Innovation Center for Biotherapy, West China Medical School, Sichuan University, Chengdu, 610041 China
Search for more papers by this authorHaokun Li
School of Pharmaceutical Sciences, Tsinghua University, Beijing, 100084 China
These authors contributed equally to this work.
Search for more papers by this authorPeng Cheng
Collaborative Innovation Center for Biotherapy, West China Medical School, Sichuan University, Chengdu, 610041 China
These authors contributed equally to this work.
Search for more papers by this authorLong Jiang
School of Pharmaceutical Sciences, Tsinghua University, Beijing, 100084 China
Search for more papers by this authorProf. Dr. Jin-Liang Yang
Collaborative Innovation Center for Biotherapy, West China Medical School, Sichuan University, Chengdu, 610041 China
Search for more papers by this authorCorresponding Author
Prof. Dr. Liansuo Zu
School of Pharmaceutical Sciences, Tsinghua University, Beijing, 100084 China
Collaborative Innovation Center for Biotherapy, West China Medical School, Sichuan University, Chengdu, 610041 China
Search for more papers by this authorAbstract
Inspired by the biogenetic origin of goniomitine, new synthetic bio-inspired fragmentation strategies for the synthesis of functionalized 2-quinolinones and indolones have been developed. Remarkable synthetic efficiency was achieved by telescoping several transformations into one-pot reactions, allowing for the direct coupling of 2-alkynyl-anilines and diazo ketones. The synthetic utility was demonstrated by the 5-step asymmetric total synthesis of (−)-goniomitine from 2-ethyl-cyclopentanone.
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