摘要/Abstract

色醇类衍生物是一类十分重要的化合物，具有广谱的药理和生理活性.报道了以1-（3-二甲氨基丙基）-3-乙基碳二亚胺盐酸盐（EDCI）和1-羟基苯并三唑（HOBt）作为缩合试剂，在温和的条件下对各种取代的色醇与β，γ-不饱和α-酮酸进行的缩合酯化反应，制备了一系列β，γ-不饱和-α-酮酸色醇酯类化合物.该方法底物适应性广，原料易得且操作简便.
关键词: 缩合试剂, 色醇, 酯化, β,γ-不饱和α-酮酸, β,γ-不饱和-α-酮酸色醇酯
Tryptophol derivatives are very important compounds with wide spectrum of pharmaceutical and physiological activity. Herein, the esterification reaction of trypthol and its derivatives with β,γ-unsaturated α-keto acids was reported by the use of 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (EDCI) and 1-hydroxybenzotriazole (HOBt) as conden-sation reagents. A series of β,γ-unsaturated α-keto trypanol ester derivatives were prepared in moderate to high yields. This method has advantages of riched functional group tolerance, readily available starting materials and easy operation.
Key words: condensation reagent, tryptophol, esterification, β,γ-unsaturated α-keto acid, β,γ-unsaturated α-keto trypanol ester


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