医药中间体尿嘧啶的合成研究

Study on the Synthesis of Uracil as a Pharmaceutical Intermediate

目的改进抗病毒和抗肿瘤等药物的重要中间体尿嘧啶的合成方法并初步探讨了用尿素替代硫脲合成尿嘧啶的可能性。方法以甲酸乙酯、乙酸乙酯为起始原料,采用一锅法合成了尿嘧啶,产物结构经1H NMR表征。结果工艺创新优化后,收率达71%,产品纯度>99%(HPLC归一化法)。结论改进后的工艺降低了成本,简单可行,适合工业化生产。

Objective To improve the synthesis of uracil which is an important pharmaceutical intermediate for antiviral, antican-cer drugs, etc, and to preliminarily discuss the feasibility of urea synthetizing uracil in place of thiourea. Methods Ethyl formate and ethyl acetate were used as the starting material to synthesize the target compound by one-pot method whose structure was identified by 1 HNMR spectrometry. Results With improved technology, the yield of product reached 71%, and the purity exceeded 99%（ HPLC, normalization method） . Conclusion The improved technology, simple and feasible, has reduced the cost, which is suitable for industrial production.