Hexafluoroisopropanol has been demonstrated as the versatile promoter for redox-neutral α-C(sp 3 )−H functionalization of cyclic amines via the cascade [1,5]hydride transfer/cyclization strategy. A wide range of cyclic amines are functionalized into bioactive tetrahydroquinolines, quinazolines, benzoxazines, and benzotriazepines in moderate to excellent yields. This protocol features additive-free conditions, operational simplicity, and wide substrate scope.
An unprecedented organocatalytic cascade aldimine condensation/[1,6]-hydride transfer/Mannich-type cyclization of indole-2-carbaldehydes with o-aminoanilines was developed to assemble polycyclic indole-2,3-fused diazocanes in one-step. This novel methodology features high step- and atom-economy, redox-neutral,...
The hydride transfer enabled the first success of the regioselective dearomatization of indoles in the carbocyclic ring and the pyrrol ring, which was induced by ortho-quinone methides and vinylogous iminium...
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