Palladium-Catalyzed Hydride Addition/C-H Bond Activation Cascade: Cycloisomerization of 1,6-Diynes

Org Lett. 2018 Nov 2;20(21):6915-6919. doi: 10.1021/acs.orglett.8b03057. Epub 2018 Oct 19.

Abstract

The use of ammonium halide salts as metal hydride precursors in a new Pd-catalyzed cycloisomerization of 1,6-diynes, which affords unexplored silylated 2-azafluorenes, is reported. This cascade process includes the addition of a Pd-hydride species to a π-system, intramolecular carbopalladation, and C(sp2)-H bond activation. A variety of functional groups are tolerated, and the synthetic utility of the resulting products has been demonstrated by a series of derivatizations.

Publication types

  • Research Support, Non-U.S. Gov't