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Access to 2,3-Disubstituted Benzofurans through One-Pot Acid-Catalyzed Nucleophilic Substitution/TBAF-Mediated Oxacycloisomerization



An efficient synthetic strategy for the synthesis of diversely 2,3-disubstituted benzofurans is described. This method is based on the use of propargylic alcohols generated from TBS-protected ortho-hydroxy benzaldehydes as starting materials and allows a library of 2,3-disubstituted benzofurans to be built. The procedure consists of one-pot nucleophilic substitution, TBS-deprotection, and exo-dig cycloisomerization.