N-tosyl-3-azacyclohexyne. Synthesis and chemistry of a strained cyclic ynamide

J Am Chem Soc. 2014 Nov 5;136(44):15489-92. doi: 10.1021/ja509055r. Epub 2014 Oct 22.

Abstract

The first synthesis of a strained six-membered cyclic ynamide is described. N-Tosyl-3-azacyclohexyne is generated via fluoride-promoted 1,2 elimination under conditions that allow trapping of the strained heterocyclic alkyne in a variety of addition, insertion, and [2 + 2], [3 + 2], and [4 + 2] cycloaddition reactions.