E-mail: dsshin@changwon.ac.krReceived December 1, 2013, Accepted February 18, 2014A facile and effective method has been developed for the synthesis of a novel series of benzofuran derivativesvia N-acylation, O-alkylation and intramolecular condensation reactions, starting from readily availablesubstituted o-hydroxy aryl ketone, and chloroacetyl arylamides. This metal-free transition process ischaracterized by mild reaction conditions, atom economy, short reaction time and a high yield with a decreasedamount of by-products.Key Words : Benzofuran, o-Hydroxy aryl ketone, Amine, Synthesis, Intramolecular condensationIntroductionBenzofuran moiety is abundant in both natural and arti-ficial molecules. Substituted benzofurans are pharmaceuti-cally important heterocycles that display numerous bio-logical activities such as antimicrobial,