溴匹立明的合成

Synthesis of Bropirimine

溴匹立明是一种治疗膀胱癌的药物。乙酰乙酸乙酯与新制备的乙醇钠反应制得乙酰乙酸乙酯钠盐,然后与苯甲酰氯反应,经过酸化、洗涤、减压蒸馏,得到苯甲酰乙酸乙酯。苯甲酰乙酸乙酯与碳酸胍进行环化反应,然后进行溴化反应,即可得到产品溴匹立明,总收率为34.6%。该合成方法操作简单,适合工业化生产。

Bropirimide is a medicine for bladder cancer.The ethyl acetoacetate is reacted with the newly prepared sodium ethoxide to obtain the ethyl acetoacetate sodium salt,which is then reacted with benzoyl chloride.After acidification,washing and distillation under reduced pressure,ethyl benzoyl acetate is obtained.Cyclization reaction between ethyl benzoyl acetate and guanidine carbonate,followed by bromination reaction,can obtain the product bropirimine,with a total yield of 34.6%.The synthetic method is simple and suitable for industrial production.