新颖的二硼类催化剂应用于合成芳基酰胺-全合成fridae羧酸和胺缩合生成酰胺是一种常见的合成反应类型陈苦 , 通常需要在缩合剂的作用完成陈善有 ,采??

新颖的二硼类催化剂应用于合成芳基酰胺-全合成fridae


羧酸和胺缩合生成酰胺是一种常见的合成反应类型陈苦 , 通常需要在缩合剂的作用完成陈善有 ,采用（二甲氨基）二硼和四羟基二硼烷作为催化剂周炜简历, 促使芳香羧酸和胺脱水缩合是一种新颖的合成策略吕媭 , 无需使用化学计量或额外的缩合剂.

芳香羧酸与游离胺很容易形成铵盐风早神人, 不利于缩合反应的发生王缇 , 这一新的合成策略可能的反应机理是归因于两个关健步骤:
(1)从相应的铵盐中解离游离胺 .
(2)通过双齿配位到B-B键分子上选择性的活化羧基.
合成方法如下:

An oven dried 20 mL RB flask equipped with magnetic stirring bar was charged withcarboxylic acid (0.5 mmol张劲东博客 , 1 equiv) and dissolved in 5 mL dry toluene阿玖春温一笑 , with subsequentaddition of amine (0.5 mmol居长龙 , 1 equiv) and catalyst (2 mol%). The resulting suspension wasstirred at reflux temperature under azeotropic condition for 7 h. After completion俞斯亮, RM wascooled to room temperature. The solvent was evaporated under reduced pressure to drynessand residue was dissolved in ethyl acetate. After the addition of H2O乔蒂·阿姆奇 ,至尊艳皇 the aqueous phase wasextracted with EtOAc (3x). The combined organic phases were washed with sat. aq. NaHCO3and brine机时小偷 , dried over Na2SO4kldby , filtered西川茂, and removed under reduced pressure. The residue waspurified by column chromatography on silica gel (n-Hexane/EtOAc) to afford the pure products.
原文: Diboron-Catalyzed Dehydrative Amidation of Aromatic CarboxylicAcids with Amines (Org. Lett.DOI: 10.1021/acs.orglett.8b01480 )

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