We report an electrophilic cyclization of alkynyl imines to afford polysubstituted 3-haloquinolines using CuX-activated N-halosuccinimdes (NXS) as electrophiles. Control experiments demonstrated that the NXS/CuX system might be more active than single NXS and could be applied in the electrophilic cyclization of electron- deficient substrates.

A facile synthesis of thiepine sulfones is described. It relies on a sequence of Rh(III)-catalyzed C-H cleavage, 1,5-H shift, and intramolecular allene insertion. As a result of extremely readily accessible starting materials and convenient operation, this protocol should be an appealing strategy in organic synthesis.