摘要
甘氨酸乙酯盐酸盐经重氮化反应制得重氮乙酸乙酯,与异丁烯在自制的手性催化剂—(R,R)-(+)-2,2′-亚异丙基双(4-叔丁基-2-噁唑啉)与三氟甲磺酸亚铜的络合物催化下进行不对称环丙烷化反应,制得(S)-2,2-二甲基环丙烷甲酸乙酯,碱性条件下水解,再与氯化亚砜反应得酰氯后氨解制得(S)-(+)-2,2-二甲基环丙烷甲酰胺,总收率约27%。
(S) -(+) -2,2-Dimethylcyclopropanecarboxamide was synthesized from ethyl glycinate hydrochloride by diazotization to give ethyl diazoacetate,which was subjected to asymmetric cyclopropanation with isobutylene in the presence of chiral bis(oxazolines) ligand and copper(Ⅰ) triflate,basic hydrolysis,acylchlorination and then aminolysis with an overall yield of about 27%.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
2011年第7期491-494,共4页
Chinese Journal of Pharmaceuticals
