一类线性β,γ-不饱和α-酮酸色醇酯类化合物的合成

Synthesis of a Type of Linear β,γ-Unsaturated α-Keto Tryptophol Ester Compounds

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.

Tryptophol derivatives are very important compounds with wide spectrum of pharmaceutical and physiological activity.Herein,the esterification reaction of trypthol and its derivatives withβ,γ-unsaturatedα-keto acids was reported by the use of 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride(EDCI)and 1-hydroxybenzotriazole(HOBt)as condensation reagents.A series ofβ,γ-unsaturatedα-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.