Rh-catalyzed, chelation-induced, C-5 regioselective C–H functionalization of 8-amidoquinolines with a range of N -Boc aminals is reported for the first time. The addition of in situ generated imines to C(sp 2 )–H bonds afforded branched amines in good to excellent yields. Moreover, this transformation features good functional group compatibility, broad substrate scope, and mild reaction conditions and is suitable for gram-scale synthesis. In addition, an unprecedented, chelation-induced, site-selective, remote dimerization of quinolines led to the formation of dimer frameworks in moderate yields under Rh-catalyzed conditions.
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Fronczek et al. (2016) studied this question.
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