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

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.