摘要/Abstract
报道了一种无过渡金属条件下，α-芳香酮酸和叠氮磷酸二苯酯（DPPA）发生脱羧偶联制备芳香伯酰胺的方法.该方法条件温和，无需惰性气体保护，各种取代芳香α-酮酸均可顺利反应得到优良的分离产率，体现了较好的官能团适应性.克量级实验在该反应条件下也可顺利实现，以高产率生成目标产物，同时对反应机理也进行了探究.
关键词: 脱羧酰胺化反应, 伯酰胺, 叠氮磷酸二苯酯, α-芳香酮酸, 无过渡金属
In this paper, a novel transition-metal-free decarboxylative amidation of aryl α-keto acids with diphenylphosphoryl azide (DPPA) under mild conditions has been developed. The reaction proceeded smoothly to afford the corresponding primary aryl amide products in good to excellent yields under air and showed excellent functional group tolerance. Gram-scale reaction was also performed to produce the desired product in high yield. In addition, the mechanism of the present reaction was investigated.
Key words: decarboxylative amidation, primary amides, diphenylphosphoryl azide, α-keto acids, transition-metal-free
PDF全文下载地址:
点我下载PDF
