苯甲酸阿格列汀关键中间体合成工艺改进

摘要

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.%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。