沙格列汀关键中间体（S）-N-叔丁氧羰基-3-羟基金刚烷基甘氨酸的合成研究进展

摘要

Saxagliptin,a novel antihyperglycemic agent belonging to dipeptidyl peptidase-4(DPP-4)inhibitor,was devel⁃oped by Bristol-Myers Squibb and AstraZeneca. It has the merit of obvious hypoglycemic activity,less side effect,good treatment com⁃pliance and remarkably high safety,and is widely applied to treatment of type 2 diabetes. In this paper,we review the synthetic meth⁃ods of the key intermediate(S)-N-Boc-3-hydroxyadamantylglycine(compound 3)as well as its two important compounds 3-hydroxy-1-acetyladamantane(1)and 2-(3-hydroxy-1-adamant-yl)-2-oxoacetic acid(2)and briefly discuss their advantages and disadvantages.%沙格列汀是一种新型抗糖尿病药物，属二肽基肽酶Ⅳ（DPP-Ⅳ）抑制剂，由Bristol-Myers Squibb和Astra Zeneca联合开发。该药降血糖作用明显，副作用小，患者顺应性好，安全性高，已被广泛用于2型糖尿病的治疗。本文综述了沙格列汀关键中间体（S）-N-叔丁氧羰基-3-羟基金刚烷甘氨酸（化合物3）及其两个重要中间化合物3-羟基-1-乙酰金刚烷（1）和2-（3-羟基-1-金刚烷基）-2-乙醛酸（2）的合成方法并对其优缺点进行了简单评述。