A facile and efficient approach for the synthesis of the CF3-containing dioxodibenzothiazepines has been developed via copper-catalyzed trifluoromethylation/cyclization of alkynes utilizing a radical relay strategy. This method has demonstrated low catalyst loading, high regiocontrol, and broad scope under mild conditions. Good compatibility for the N-protecting group, gram-scale experiment, and further derivation of product prove the versatility of this transformation.

The cross-coupling of C−N bond directly from inert C−H bonds is an ideal approach to synthesize saturated azacycles due to its high efficiency and atom economy. In this article, a copper-catalyzed intramolecular amination via the cross coupling of C(sp 3 )−H and N−H bonds of secondary amine has been reported, which exhibit excellent chemo-and regioselectivity, extensive substrate scope, and functional group tolerance in good to excellent yield, offering an efficient pathway to build nitrogen-containing heterocycle skeletons.Letter pubs.acs.org/OrgLett

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