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One-Pot Synthesis of 2,3-Diarylbenzofurans via Sequential Iodocyclization and Pd-Catalyzed Suzuki Coupling Reactions of 2-Alkynylanisoles with Boronic Acids in Water
Authors:Jiang-Sheng Han  Su-Qin Chen  Ping Zhong
Affiliation:1. College of Chemistry and Materials Engineering , Wenzhou University , Wenzhou , China;2. ShanDong WeGo Pharmaceutical Co. Ltd., Wego Group , Weihai , China;3. College of Chemistry and Materials Engineering , Wenzhou University , Wenzhou , China;4. Oujiang College, Wenzhou University , Wenzhou , China
Abstract:An efficient approach for the one-pot synthesis of 2,3-diarylbenzofurans via sequential iodocyclization and Pd-catalyzed Suzuki coupling reaction of 2-alkynylanisoles with boronic acids in water is reported. The protocol utilizes water as the solvent and there is no need to isolate the intermediate 3-iodine-2-arylbenzofurans, which exemplifies the ideal of green chemistry. Various 2-alkynylanisoles and boronic acids can participate in the reactions, providing a series of 2,3-diarylbenzofurans for drug discovery in moderate to good yields.
Keywords:2-Alkynylanisole  boronic acid  2,3-diarylbenzofuran  iodocyclization  palladium  Suzuki coupling reaction
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