- Synthesis of CF3CH2-Containing Indolines by Transition-Metal-Free Aryltrifluoromethylation of Unactivated Alkenes
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With an unactivated double bond as the radical acceptor, allyl amines underwent a metal-free trifluoromethylation/cyclization cascade with CF3SO2Na (Langlois' reagent), affording CF3CH2-containing indolines and tetrahydroisoquinolines, whose practical syntheses are significant challenges. This protocol features mild conditions, low cost, and a broad substrate scope.
- Liang, Deqiang,Dong, Qishan,Xu, Penghui,Dong, Ying,Li, Weili,Ma, Yinhai
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supporting information
p. 11978 - 11986
(2018/09/27)
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- Synthetic method of CF3-containing indoline and 1,2,3,4-tetrahydroisoquinoline
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The invention discloses a synthetic method of CF3-containing indoline and 1,2,3,4-tetrahydroisoquinoline and relates to the technical field of compound synthesis. The synthetic method herein is basedon metal-free trifluoromethylation/cyclization free radical cascade reaction using a nonactive olefin dual-bond as a free radical receptor; the reaction aforementioned helps synthesize, in one step, CF3-containing indoline and 1,2,3,4-tetrahydroisoquinoline. The synthetic method herein has the significant advantages of mild conditions, good operational simplicity, low cost, wide substrate range, good exo selectivity and the like.
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Paragraph 0027; 0029; 0030; 0031; 0042
(2019/01/14)
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