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以4-哌啶甲酸和乙醇为原料,分别通过与二氯亚砜和三甲基氯硅烷反应两种不同的酯化方法制备药物中间体4-羧酸乙酯哌啶,产率分别为85.0%和92.7%,纯度均达到99%。并讨论了三甲基氯硅烷用量及反应温度等因素对反应的影响,获得了适宜的反应条件。
4-piperidinecarboxylic acid and ethanol were used as starting materials to prepare ethyl 4-carboxylate piperidine, respectively, by two different esterification methods with thionyl chloride and trimethylchlorosilane. The yields were 85.0 % And 92.7%, purity of 99%. The influences of the dosage of trimethylchlorosilane and the reaction temperature on the reaction were discussed. The suitable reaction conditions were obtained.