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Simple,Convenient, and Efficient Synthesis of 2-Aryl-substituted Benzo[b]furans
Authors:Yong Jiang  Botao Gao  Wenjuan Huang  Yongmin Liang  Yongxiang Ma
Institution:State Key Laboratory of Applied Organic Chemistry, Lanzhou University , Lanzhou, China
Abstract:A simple, convenient, and efficient one-pot method for the preparation of benzofuran is reported. Sonogashira coupling reaction of aryl iodides with 2-methyl-3-butyn-2-ol was used as an acetylene source in the presence of Pd(PPh3)2Cl2 and CuI. Deprotection of the acetylene moiety in the same pot using a strong base and the second Sonogashira coupling/cyclization of and substituted o-iodophenols led to the formation of the appropriate benzob]furans. These protocols also can be used in the synthesis of natural products and indoles.
Keywords:Aryl iodide  benzo[b]furan  2-methyl-3-butyn-2-ol  o-iodophenol  Sonogashira reaction
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