西他列汀中间体2-甲基-N-(2-(2,4,5-三氟苯乙酸)亚乙基)丙烷-2-亚磺酰胺的合成  

Synthesis of the Synthetic Intermediate of Sitagliptin(R,E)-2-methyl-N-(2-(2,4,5-trifluor-ophenyl)ethylidene)propane-2-sulfinamide

作　　者：刘小卒[1] 韦文陶 Liu Xiaozu;Wei Wentao(Pharmacy school,Zunyi medical university,Zunyi 563000,China)

机构地区：[1]遵义医学院药学院,贵州遵义563000

出　　处：《广东化工》2018年第16期42-43,共2页Guangdong Chemical Industry

摘　　要：以2,4,5-三氟苯甲醛为原料,经Wittig反应、(R)-(-)-叔丁基亚磺酰胺缩合得到中间体(R,E)-2-methyl-N-(2-(2,4,5-trifluor-ophenyl)ethylidene)propane-2-sulfinamide。新的合成工艺有以下优点:采用Wittig反应合成烯醇醚,并应用于亚磺酰胺缩合反应,避免了不稳定的2-(2,4,5-三氟苯基)乙醛的使用,提高了产率,缩短了合成路线。产物及中间体的结构经1H NMR确认。The chiral（R,E）-2-methyl-N-（2-（2,4,5-trifluor-ophenyl）ethylidene）propane-2-sulfinamide, an intermediate of sitagliptin, was prepared through a Wittig reaction followed by condensation with（R）-tert-butylsulfinamide. The utilization of Wittig reaction for synthesis of enol ether and subsequent condensation rendered this synthetic route more efficient and concise than previous works. The structures of product and intermediate have been confirmed by 1 H NMR.

关 键 词：西他列汀 WITTIG反应 (R)-(-)-叔丁基亚磺酰胺 缩合反应 

分 类 号：TQ460.4[化学工程—制药化工]