Development of Cyanopyrazoles as Building Blocks to Fungicide Fluxapyroxad and Analogues

J Org Chem. 2019 Jun 7;84(11):7148-7158. doi: 10.1021/acs.joc.9b00819. Epub 2019 May 15.

Abstract

Herein, we present a facile approach to a diverse collection of 1,4-disubstituted 3-di- or mono-fluoromethylpyrazoles utilizing our previously developed cyanopyrazoles as key building blocks. This method features several merits, such as easily accessible starting materials, broad substrate scope, mild reaction conditions, and simple operation. This protocol further deserves to be highlighted by the successful translation into the synthesis of commercialized fungicide fluxapyroxad and its analogues.

Publication types

  • Research Support, Non-U.S. Gov't