American Chemical Society
ol4032254_si_003.cif (13.41 kB)

Benzofuran Derivatives from Alkynyl-Substituted Benzynes and Aryl Halides

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posted on 2014-01-03, 00:00 authored by Weiming Yuan, Shengming Ma
A palladium(0)-catalyzed cascade reaction for the efficient synthesis of 2,3-disubstituted benzofuran derivatives 3 containing a 3-trisubstituted alkene functional group in moderate yields from alkynyl-substituted benzynes 1 and aryl halides 2 has been developed. This method provides an efficient and alternative approach to benzofurans which are very useful heterocyclic compounds with biological and pharmacological potentials. A plausible mechanism involving intramolecular ene reaction, intermolecular insertion, and β-H elimination is proposed.