Benzofuran derivatives from alkynyl-substituted benzynes and aryl halides
1Shanghai Key Laboratory of Green Chemistry and Chemical Process, Department of Chemistry, East China Normal University , 3663 North Zhongshan Lu, Shanghai 200062, P. R. China.
Abstract:
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.
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