申请人:I.S.F. Spa
公开号:US04124594A1
公开(公告)日:1978-11-07
Pyrrolidine derivatives of the formula ##STR1## are prepared from .gamma.-amino-.beta.-hydroxybutyric acid which, after reaction with a silylating agent, is reacted, in the presence of an acid acceptor, with a halogen derivative of an ester of an aliphatic acid and then cyclized to give the corresponding N-alkoxy-carbonylalkyl derivative which is converted into the corresponding amide by treatment with ammonia or with a mono- or di-substituted amine. The compounds produced by the present invention improve learning memory and display a protecting effect against the E.E.G. consequence of an overdose of barbituates and against the reduced performance following brain damage (e.g. cerebral edema).
本发明提供了公式##STR1##的吡咯烷衍生物的制备方法。该方法从γ-氨基-β-羟基丁酸出发,经过硅基化试剂反应后,在酸受体的存在下,与脂肪族酸酯的卤代衍生物反应,然后环化,形成相应的N-烷氧基-羰基烷基衍生物,再通过与氨或单取代或二取代胺处理,转化为相应的酰胺。本发明所制备的化合物可以提高学习记忆能力,并对巴比妥类过量引起的脑电图后果和脑损伤(如脑水肿)后的性能下降具有保护作用。