Hexafluoroisopropanol has been demonstrated as the versatile promoter for redox-neutral α-C(sp)-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.
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| http://dx.doi.org/10.1021/acs.joc.9b02606 | DOI Listing |
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