苯甲酸阿格列汀关键中间体合成工艺改进  

Improved Synthesis of the Key Intermediate of Alogliptin Benzoate

作　　者：高尚[1] 俞传明[1] 何人宝 金逸中 

机构地区：[1]浙江工业大学药学院长三角绿色制药协同创新中心绿色制药技术与装备教育部重点实验室,浙江杭州310014 [2]浙江永太科技股份有限公司,浙江临海317016

出　　处：《浙江化工》2016年第2期17-19,共3页Zhejiang Chemical Industry

摘　　要：报道了苯甲酸阿格列汀的关键中间体(R)-2-[(6-(3-Boc-氨基哌啶-1-基)-3-甲基-2,4-二氧代-3,4-二氢嘧啶-1(2H)-基)甲基]苄腈的合成方法,通过优化反应溶剂和缚酸剂,改进投料用量,有效避免了反应杂质生成的同时降低了反应成本,使路线更加适合工业化生产。A new method was reported for synthesis of 2-（{6-[（3R）-3-Boc-piperidin-1-y-l]-2,4-dioxo-1,2,3,4-tetrahydropyrimidin-1-yl}methyl）benzonitrile, which is the key intermedi-ate of Alogliptin benzoate.Being well optimized, the improved process has the merits of low cost, less impurities and simple operation to meet the needs of industrial production.

关 键 词：苯甲酸阿格列汀 中间体 异丙醇 工艺优化 

分 类 号：TQ463[化学工程—制药化工]