四氢吡咯,4-溴-2,6-二氟苯甲酸置于1-羟基苯并三唑,盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺,N,N-二异丙基乙胺,(1,1'-Bis(Diphenylphosphino)Ferrocene)Palladium(II) Dichloride,Potassium Acetate,联硼酸频那醇酯,盐酸,Sodium Periodate体系中,用 乙腈,2-甲基四氢呋喃,水 作为反应溶剂,以48%的收率获得产物玉米醇溶蛋白
参考文献:A Robust Three-Step Telescoped Synthesis Of Electron-Deficient Amide Substituted Arylboronic Acids
标题:A Robust Three-Step Telescoped Synthesis Of Electron-Deficient Amide Substituted Arylboronic Acids
摘要:A Robust Three-Step Telescoped Process For The Preparation Of Electron-Deficient Amide-Substituted Arylboronic Acids From Readily Available Bromobenzoic Acids Has Been Developed. An Edc-Hobt-Promoted Amide Formation Of A Bromobenzoic Acid Was Followed By Subjection Of The Product Stream To A Palladium-Mediated Cross-Coupling With B-2(Pin)(2). The Resultant Mixture Of The Arylboronate Ester And Arylboronic Acid Was Directly Treated With Naio4,Followed By A Heptane-Methf Crystallization,To Cleanly Afford The Corresponding Arylboronic Acid In Good Yield. This General Procedure Was Used To Synthesize Electron-Deficient Amide-Substituted Arylboronic Acids With A Diverse Array Of Electron-Withdrawing Substituents.
DOI:10.1021/op100267P