2-(3-羟基-1-金刚烷基)-2-乙醛酸的合成  

Synthesis of 2-(3-Hydroxy-1-adamantyl)-2-glyoxylic Acid

作　　者：李靖柯[1] 周鸿睿[1] 彭俊[1] 冯悦[1] 胡湘南[1] 

机构地区：[1]重庆医科大学药学院,重庆400016

出　　处：《中国医药工业杂志》2012年第4期251-253,共3页Chinese Journal of Pharmaceuticals

基　　金：重庆市自然科学基金(2006BB5286)

摘　　要：金刚烷经相继甲酸化、酰氯化后与丙二酸二乙酯乙氧基镁反应,得到1-金刚烷甲酰基丙二酸二乙酯,再经水解脱羧、高锰酸钾氧化得到沙克列汀中间体2-(3-羟基-1-金刚烷基)-2-乙醛酸,总收率约28%。2-（3-Hydroxy-l-adamantyl）-2-glyoxylic acid, the intermediate of saxagliptin, was synthesized from adamantane via successive reactions with formic acid, thionyl chloride and diethyl ethoxymagnesium malonate to give diethyl 1-adamantaneformyl malonate, which was subjected to hydrolysis and decarboxylation by mixed acid and then oxidation by potassium permanganate. The overall yield was about 28 %.

关 键 词：2-(3-羟基-1-金刚烷基)-2-乙醛酸 沙克列汀 2型糖尿病 中间体 合成 

分 类 号：O624.5[理学—有机化学]