| abstract |
The invention discloses a synthesis method of sitagliptin and its salts. Using 2,4,5-trifluorophenylacetic acid as a starting material, after esterification, reduction, oxidation and Witting reactions, 4-(2 , 4,5-trifluorophenyl)-2-butene ethyl ester, or 4-(2,4,5-trifluorophenyl)-2-butene ethyl ester after reduction, oxidation and Witting reaction . Then, under the action of butyllithium or sodium hexamethyldisilazane, it undergoes hydroamination reaction with chiral amine to construct the chiral hydroamination product, and then undergoes three steps of ester hydrolysis, condensation and hydrogenation to obtain cetaxel Ting. The raw materials of the synthesis method of sitagliptin are cheap and easy to obtain, the steps are few, the operation is easy, and the cost can be effectively reduced. The method can obtain high-purity sitagliptin, and the HPLC purity and ee value of the sitagliptin phosphate obtained after salt formation are both above 99%, and can be applied in the field of medicine. |