A One-Pot Construction of Halogenated Trifluoromethylated Pyrroles through NXS (X = Br, I) Triggered Cascade

Org Lett. 2017 Sep 15;19(18):4968-4971. doi: 10.1021/acs.orglett.7b02427. Epub 2017 Sep 1.

Abstract

An easy two-step, one-pot synthesis of halogenated trifluoromethylated pyrroles is realized by sequential intermolecular hydroamination reaction of 2-trifluoromethyl-1,3-enynes with aliphatic primary amines under mild reaction conditions, and NXS mediated oxidative cyclization of the hydroamination product. The salient features of this method include mild conditions, readily available starting materials, general substrate scope, high efficiency and synthetic utility of the products.

Publication types

  • Research Support, Non-U.S. Gov't