A convergent formal [4 + 2] cycloaddition of 1,6-diynes and benzyl azides: construction of spiro-polyheterocycles

Abstract

A convergent formal [4 + 2] cycloaddition reaction for the construction of structurally appealing spiro-tetrahydroquinolines has been developed, in which, a one-pot reaction is established for the in situ generation of two reagents, a cyclic alkyne and an N-aryliminium ion, from the corresponding precursors in the presence of an Au-catalyst and Brønsted acid, respectively.