摘要
金刚烷甲酮(2)经高锰酸钾两步氧化制得糖尿病药物沙格列汀中间体2-(3-羟基-1-金刚烷)-2-氧代乙酸,总收率为74.7%:氧化条件①以溴化四丁铵为相转移催化剂,高锰酸钾与2投料摩尔比2.05∶1,反应温度50～55℃、pH12～13;②续加1.2当量的高锰酸钾,温度40～45℃,pH 8～9。
2-（3-Hydroxy-l-adamantane）-2-oxoacetic acid, the intermediate of saxaglipitin for type 2 diabetes, was synthesized from adamantyl methyl ketone （2） via two-step oxidation by potassium permanganate with an overall yield of about 74.7% ： （1）the molecular ratio of potassium permanganate and 2 was 2.05 ： 1, the temperature was controlled at 50 - 55 ℃ with tetrabutylammonium bromide as catalyst, and the pH value was adjusted to 12 - 13; （2） additional 1.2 eq potassium permanganate was added, the temperature was controlled at 40 - 45 ℃ and the pH value was adjusted to 8 - 9.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
2013年第3期233-234,共2页
Chinese Journal of Pharmaceuticals
基金
浙江省高校优秀青年教师资助项目(00511024)
