Synthesis of arylsulfonyl-substituted indolo[2,1-a]isoquinolin-6(5H)-one derivatives via a TBAI-catalyzed radical cascade cyclization |
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| Institution: | 1. College of Chemistry & Environmental Engineering, Anyang Institute of Technology, Anyang 455000, China;2. Department of Chemistry, Guangdong University of Education, Guangzhou 510303, China;3. State Key Laboratory of Chemical Oncogenomics and Key Laboratory of Chemical Genomics, Shenzhen Engineering Laboratory of Nano Drug Slow-Release, Shenzhen Graduate School of Peking University, Shenzhen 518055, China |
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| Abstract: | We have developed a metal-free radical cascade reaction of N-substituted 2-aryl indoles with readily available sulfonyl hydrazides for the rapid construction of arylsulfonyl-substituted indolo2,1-a]isoquinolin-6(5H)-one derivatives. With the TBAI–TBHP catalytic system, a broad series of structurally diverse indolo2,1-a]isoquinolin-6(5H)-one derivatives were obtained in moderate to excellent yields. The reaction features mild reaction conditions, operationally easiness, scaled-up feasibility, and high functional-group-tolerance. |
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