摘要
通过合成路线的改进以及合成工艺的优化,方便高效地得到了抗高血压药物群多普利的关键中间体(2S,3aR,7aS)-八氢-1H-吲哚-2-甲酸苄酯.产品结构及绝对构型通过NMR及HPLC进行表征,与文献报道的数据完全一致.最终以99%的对映选择性及13.2%的产率得到目标化合物.为群多普利关键中间体的合成提供了一条可工业化的途径.
The key intermediate of antihypertensive drugs trandolapril, （2S,3aR,7aS）-benzyl octahydro-lH-indole-2-car- boxylate, was synthesized by improvement of synthetic route and optimation of synthetic technology with satisfactory results （99% ee and 13.2% overall yield）. The structure and absolute configuration of the product were characterized by NMR and HPLC analysis, which are completely consistent with the reported data of the literature. It was obvious that the current meth- odology provided an efficient pathway for the synthesis of trandolapril.
出处
《有机化学》
SCIE
CAS
CSCD
北大核心
2013年第7期1573-1577,共5页
Chinese Journal of Organic Chemistry
基金
国家自然科学基金(Nos.21172143
21172145
21232004)资助项目~~
