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 %.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
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)
