Controlled Dimroth Rearrangement in the Suzuki-Miyaura Cross Coupling of Triazolopyridopyrimidines

J Org Chem. 2016 Dec 16;81(24):12506-12513. doi: 10.1021/acs.joc.6b02357. Epub 2016 Dec 5.

Abstract

Polynitrogen heterocycles are often subject to Dimroth rearrangement which consists of ring opening, bond rotation, and ring closure. In this note, we report a synthesis of two new families of triazolopyridopyrimidines. Successful functionalization via a Suzuki-Miyaura coupling was performed with total control of triazole (Dimroth) isomerization based on the judicious choice of reaction conditions.

Publication types

  • Research Support, Non-U.S. Gov't