AlCl 3 induced C-arylation/cyclization in a single pot: A new route to benzofuran fused N-heterocycles of pharmacological interest

Abstract

A new and one-pot synthesis of benzofuran fused N-heterocycles has been accomplished via AlCl 3-mediated C-C followed by C-O bond formation between 2,3-dichloropyrazine or its derivatives and phenols. The methodology provided novel compounds as potential inhibitors of PDE4B. The single crystal X-ray data of a synthesized benzofuran derivative are presented. Scope of the methodology, in vitro pharmacological data of some of the synthesized compounds, along with docking study of an active compound are described. © 2011 Elsevier Ltd. All rights reserved.