磷酸西他列汀的合成路线设计摘要：第一个能够对Ⅱ型糖尿病中的二肽基肽酶-Ⅳ（DPP-4）起到治疗作用的抑制剂药物是磷酸西他列汀，它是由默克公司进行研究发现的。本药品可以控制血糖，再加以控制饮食和运动效果更佳。本文通过分析对比国内外有关磷酸西他列汀的资料，查找其的合成步骤，并而且以文献的案例为参考，以 2,4,5-三氟苯乙酸和以 2,4,5-三氟苄溴为起始原料两种方法，探索设计出一条以 2,4,5-三氟苯乙酸作为起跑点，然后把 3-氧代-4-（2,4,5-三氟苯基）丁酸乙酯当做中间点，使得它们二者产生反应，从而制造出磷酸西他列汀，这是一条新的磷酸西他列汀生产路线，为磷酸西他列汀的生产应用提供参考。关键词：磷酸西他列汀；合成；2,4,5-三氟苯乙酸；2,4,5-三氟苄溴Synthetic route design of Sitagliptin phosphate monohydrateAbstract：Sisalectin phosphate, developed by Merck, is the first drug of the class of dipeptidyl peptidase-IV (DPP-4) inhibitors for the treatment of type 2 diabetes. This medicine can control blood sugar, and then control diet and exercise better. This paper analyzes and compares the synthesis methods of sitagliptin phosphate in domestic and foreign literatures, and references 2,4,5-trifluorophenylacetic acid and 2,4,5-trifluorobenzyl bromide in the literature. Two methods of raw materials, and explored the design of an intermediate of 2-oxo-4-(2,4,5-trifluorophenyl)butanoate with 2,4,5-trifluorophenylacetic acid as the starting material. A new route for the synthesis of sitagliptin phosphate provides a reference for the production of sitagliptin phosphate.Keywords:sitagliptin phosphate; synthesis; 2,4,5-trifluorophenylacetic acid; 2,4,5-trifluorobenzyl bromide目录1 绪论.....................................................................................................................................11.1 抗糖尿病药物的研究进展.......................................................................................12 磷酸西他列汀的概述................................................
