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α-羟基酰胺类化合物具有独特的药理和生理活性,引起了有机化学家和药物化学家的广泛关注.目前,这类化合物的合成主要是通过α-羟基苯乙酸的胺基化反应,或者是通过还原α-羰基酰胺类化合物而得到.本工作通过在KOH-DMSO(二甲基亚砜)体系中,利用空气为氧化剂,发展了一种简单高效地制备α-羟基酰胺类化合物的方法.共得到21个α-羟基酰胺产物,并对这些化合物进行了结构表征,其中N-对甲苯基-2-(2-溴苯基)-2-羟基乙酰胺(2a)的结构还通过X射线单晶衍射分析确认.
The unique pharmacological and physiological activities of α-hydroxyamides have aroused widespread concern among organic chemists and drug chemists. At present, the synthesis of these compounds is mainly through the amination of α-hydroxyphenylacetic acid, or Obtained by reduction of a-carbonyl amides.This work has developed a simple and efficient method for the preparation of α-hydroxy amides by using air as oxidant in KOH-DMSO (dimethyl sulfoxide) system. A total of 21 α-hydroxyamide products were obtained and the structures of these compounds were characterized. The structure of N-p-tolyl-2- (2-bromophenyl) -2-hydroxyacetamide (2a) Single crystal diffraction analysis confirmed.