摘要
３－苄胺基丙酸乙酯（４）经Ｎ－烷基化、Ｄｉｅｃｋｍａｎｎ环合、脱羧、成肟与催化氢化５步反应得到３－氨基－１－苄基吡咯烷（９），收率３７．５％。由９分别合成了３－氨基吡咯烷二盐酸盐（１）与３－乙酰胺基吡咯烷（２），总收率从丙烯酸乙酯计分别为３０％与２０％。
Amino-1-benzylapyrrolidine(9) was synthesized starting from ethyl 3-benzylaminopropionate(4)in 37.5% overall yield via N alkylation, Dieckmann cyclization,decarboxylation,oximation and catalytic hydrogenation. 3-Aminopyrrolidine dihydrochloride(1) and 3-acetamidopyrrolidine(2) were prepared from 9 in 30% and 20% total yield based on ethyl acrylate,respectively.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
1995年第2期86-88,共3页
Chinese Journal of Pharmaceuticals
关键词
N-烷基化
乙酰胺基吡咯烷
氨基吡咯烷
合成
N-alkylation,3-aminopyrrolidine dihydrochloride,3-acetamidopyrrolidine
