Synthesis of Pyrrole-2-carbaldehyde Derivatives by Oxidative Annulation and Direct Csp3-H to C═O Oxidation

Org Lett. 2018 Feb 2;20(3):688-691. doi: 10.1021/acs.orglett.7b03821. Epub 2018 Jan 12.

Abstract

An efficient and practical de novo synthesis of pyrrole-2-carbaldehyde skeletons featuring oxidative annulation and Csp3-H to C═O oxidation is presented, exemplified by the preparation of pyrrole-2-carbaldehyde derivatives from aryl methyl ketones, arylamines, and acetoacetate esters. Preliminary mechanistic investigations indicate that the aldehyde oxygen atom originates from oxygen. Moreover, the developed scalable approach provides a distinct advantage over traditional oxidative functionalization of C-H moieties, avoiding the use of stoichiometric quantities of hazardous oxidants.

Publication types

  • Research Support, Non-U.S. Gov't