芳腈化反应中水溶剂和微波技术应用-application of water solvent and microwave technology in aromatization reaction.docxVIP

controlled microwave heating under sealed-vessel conditions has been shown to dramatically reduce reaction times, increase product yields, and enhance product purities by reducing unwanted side reactions compared to conventional synthetic methods. The many advantages of this enabling technology have not only been exploited for organic synthesis(MAOS) and in the context of medicinal chemistry/drug discovery, but also penetrated fields such as polymer synthesis, material sciences, nanotechnology, and biochemical processes.Research in our laboratory has been focused around the application of water as a solvent for the cyanation of aryl halides, particularly in conjunction with the use of microwave heating as a tool for preparative chemistry and K4[Fe(CN)6] as a cyanidesource：Cu-catalyzed cyanation of aryl halides with nontoxic K4[Fe(CN)6] was improved to be more economical and environmentally friendly by the use of water solvent and ligand-free catalyst. The reactions can be performed without any inert gas protection, which makes them more easy-handling. In addition, the suggested methodology is applicable to cyanation of a wide range of aryl iodides and activated aryl bromides, and allows the catalyst to be reused six times with a very slight change in the catalytic activity.A practical and environmentally benign methodology for Cu-catalyzed cyanation of aryl halides was well developed with some main innovations: the use of water as the solvent and ligand-free Cu(OAc)2·H2O as the catalyst under microwave heating. The suggested methodology was applicable to a wide range of substrates including aryl iodides and activated aryl bromides. In addition, the cyanated product could be quantitatively separated from the reaction mixture, and the recovered aqueous phase containing the catalyst could be reused for six times with a very slight change in the catalytic activityKEY WORDS: Cyanation, Aryl halides, Cyanide sources, Copper-catalyzed , Microwave-assisted organic synthesis