Brine G A, Boldt K G
J Pharm Sci. 1983 Jun;72(6):700-2. doi: 10.1002/jps.2600720627.
Six derivatives of 3,3-diphenyl-2-pyrrolidone were synthesized and screened for anticonvulsant activity. The synthetic route involved a mono-N-demethylation of an intermediate N,N-dimethylaminonitrile with methyl chloroformate followed by cleavage of the carbamate group. Of the six derivatives, (+/-)-2-imino-1,5-dimethyl-3,3-diphenylpyrrolidine hydrochloride was effective in protecting mice against maximal electroshock (MES) -induced seizures at a 30-mg/kg dose level.
合成了3,3-二苯基-2-吡咯烷酮的六种衍生物，并对其抗惊厥活性进行了筛选。合成路线包括用氯甲酸甲酯对中间体N,N-二甲基氨基腈进行单-N-去甲基化，然后裂解氨基甲酸酯基团。在这六种衍生物中，(±)-2-亚氨基-1,5-二甲基-3,3-二苯基吡咯烷盐酸盐在30mg/kg剂量水平下能有效保护小鼠免受最大电休克（MES）诱导的惊厥。
