苯甲酸阿格列汀合成研究进展

The Synthesis Research Progress of Alogliptin Benzoate

介绍了苯甲酸阿格列汀的药学背景,从起始原料出发总结和归纳了苯甲酸阿格列汀的现有合成路线,并对每条路线进行了分析和总结。苯甲酸阿格列汀合成的主要起始原料有6-氯尿嘧啶、6-氯-3-甲基尿嘧啶、1-(2-异氰苄基)-3-甲基脲、丙二酸单乙酯和4-甲氧基-3-氧代丁腈。认为路线以6-氯-3-甲基尿嘧啶为起始原料,反应条件温和,后处理简单,更加符合工业化生产的要求。但应进一步优化反应条件,减少副反应发生,降低成本。

In this article,pharmaceutical background of alogliptin benzoate was generalized at first.Then current different synthetic processes of alogliptin benzoate were generalized and analyzed from starting raw material such as 6-chloro uracil,6-chloro-3-methyl uracil,1-(2-isocyano benzyl)-3-methyl urea,ethyl hydrogen malonate and 4-methoxy-3-oxobutanenitrile.The route with 6-chloro-3-methyl uracil as starting raw materials showed more favorable and commercial value in the manufacturing scale such as mild reaction conditions and simple post-processing,but the reaction conditions should be further optimized to reduce side effects and cost.