Synthesis of(S)-N-Boc-3-hydroxyadamantylglycine a key intermediate of saxagliptin:research advances / 国际药学研究杂志

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.