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Updated: Jan 29, 2026
![Cercosporin-Photocatalyzed [4+1]- and [4+2]-Annulations of Azoalkenes Under Mild Conditions](/_next/image?url=https%3A%2F%2Fcloudfront.jove.com%2FCDNSource%2Fteasers%2F60786.jpg&w=3840&q=50)
Cercosporin-Photocatalyzed [4+1]- and [4+2]-Annulations of Azoalkenes Under Mild Conditions
Published on: July 17, 2020
Cu-Catalyzed [4+1] Annulation toward Indolo[2,1-a]isoquinolines through Oxidative C(sp3 )/C(sp2 )-H Bond
Tian-Shu Zhang1, Qi Zhao1, Wen-Juan Hao1
1School of Chemistry and Materials Science, Jiangsu Normal University, Xuzhou, 221116, P. R. China.
Abstract:
A Cu-catalyzed [4+1] annulation of N-aryl-1,2,3,4-tetrahydroisoquinolines (N-aryl THIQs) with α-diazoketones has been established under oxidative conditions, leading to the construction of a series of indolo[2,1-a]isoquinolines with generally good yields. The reaction enables dediazotized dicarbonylation of α-diazoketones, creating direct C(sp3 )/C(sp2 )-H bond bifunctionalization to access tetracyclic aza-heterocyclic skeletons.
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