申请人:UCB Societe Anonyme
公开号:US04837223A1
公开(公告)日:1989-06-06
(S)-alpha-ethyl-2-oxo-1-pyrrolidineacetamide, its preparation and pharmaceutical compositions containing the same. It can be prepared either by reacting (S)-alpha-ethyl-2-oxo-1-pyrrolidineacetic acid successively with an alkyl haloformate and with ammonia, or, by cyclizing an (S)-2-amino-butanamide of the formula X--CH.sub.2 CH.sub.2 -NHCH (C.sub.2 H.sub.5)CONH.sub.2 wherein Y is a --CH.sub.2 --radical when X represents a ZOOC--radical and Y is a --CO-- radical when X represents a HalCH.sub.2 --radical, Z being a C.sub.1 -C.sub.4 alkyl radical and Hal a halogen atom. This laevorotatory enantiomer has been found to have significantly higher protective activity against hypoxia and ischemia than the corresponding racemate.
(S)-α-乙基-2-氧代-1-吡咯烷乙酰胺,其制备方法和含有该化合物的药物组合物。它可以通过将(S)-α-乙基-2-氧代-1-吡咯烷乙酸先与烷基卤甲酸酯反应,然后再与氨反应来制备,或者通过将公式为X-CH.sub.2 CH.sub.2 -NHCH(C.sub.2 H.sub.5)CONH.sub.2的(S)-2-氨基丁酰胺环化得到,其中当X代表ZOOC-基团时,Y为--CH.sub.2--基团,当X代表HalCH.sub.2-基团时,Y为--CO--基团,其中Z为C.sub.1-C.sub.4烷基基团,Hal为卤素原子。这种左旋异构体已被发现具有比相应的混合物更高的保护缺氧和缺血的活性。