Synthesis of 3,4-diarylsubstituted hexahydro-1H-indoles

被引:2
作者
Zhou, Feilong [1 ,2 ]
Zhao, Erbao [1 ,2 ]
Yan, Ziqin [2 ]
Chen, Deheng [2 ,3 ]
Zhao, Yujun [2 ]
机构
[1] Univ Sci & Technol China, Nano Sci & Technol Inst, Suzhou 215123, Jiangsu, Peoples R China
[2] Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China
[3] Univ Chinese Acad Sci, Beijing 100049, Peoples R China
基金
中国国家自然科学基金;
关键词
Aziridine; Hypersaturated indole; Cation; Allylic cation; Cyclization; MISCELLANEOUS ALKALOIDS; BUILDING-BLOCKS; SCELETIUM; CONSTRUCTION; AZIRIDINES; INHIBITORS; POTENT; OCTAHYDROINDOLES; AMARYLLIDACEAE; IMIDAZOLE;
D O I
10.1016/j.tetlet.2018.04.008
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
Efficient syntheses of 3,4-diarylsubstituted hexahydro-1H-indoles in good yields with excellent diastere-oselectivities 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-C double bonds. (C) 2018 Elsevier Ltd. All rights reserved.
引用
收藏
页码:1871 / 1874
页数:4
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