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目的为了更好地对琥珀酸曲格列汀的原料药进行质量控制,合成琥珀酸曲格列汀的有关物质。方法以1-甲基巴比妥酸为起始原料,经氯代、取代反应得到有关物质A,A再经缩合,取代制得有关物质B,B再经一步反应得到有关物质C。结果与结论有关物质A、B、C的结构经1H-NMR和MS谱确证,本文首次报道了有关物质B和C的合成路线,该路线反应条件温和、操作简单。合成的有关物质可以作为琥珀酸曲格列汀原料药质量控制的对照品。
OBJECTIVE To synthesize the related substances of trastagliptin succinate in order to better control the quality of the raw drug of tratinogliolate succinate. Methods 1-methylbarbituric acid as starting material, the chlorine, the substitution reaction to obtain the relevant substances A, A and then by condensation, the replacement of the relevant substances B, B and then by a reaction to obtain the relevant substance C. RESULTS AND CONCLUSIONS The structures of A, B and C were confirmed by 1H-NMR and MS spectra. The synthetic routes for B and C were firstly reported in this paper. The reaction conditions are mild and the operation is simple. Synthesis of related substances can be used as succinate acid quality control reference substance.