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Synthesis of 3,4-diarylsubstituted hexahydro-1H-indoles |
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| Authors: | Feilong Zhou Erbao Zhao Ziqin Yan Deheng Chen Yujun Zhao | |
| Affiliation: | 1. Nano Science and Technology Institute, University of Science and Technology of China, Suzhou, Jiangsu 215123, China;2. State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zuchongzhi Rd., Shanghai 201203, China;3. University of Chinese Academy of Sciences, Beijing 100049, China | |
| Abstract: | Efficient syntheses of 3,4-diarylsubstituted hexahydro-1H-indoles in good yields with excellent diastereoselectivities were achieved with a two-step protocol comprising an allylic cation mediated nucleophilic addition and an intramolecular cyclization reaction. The N-aryl sulfonyl protecting groups of cyclization products were readily removed to furnish free amines with retention of halogen substitutions and C | |
| Keywords: | Aziridine Hypersaturated indole Cation Allylic cation Cyclization | |
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