Synthesis and Anticonvulsant Screening of 3,3 -Diphenyl- 2 -pyrrolidone Derivatives
作者:George A. Brine、Karl G. Boldt
DOI:10.1002/jps.2600720627
日期:1983.6
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
合成了6种3,3-二苯基-2-吡咯烷酮衍生物,并筛选了其抗惊厥活性。合成途径涉及中间体N,N-二甲基氨基腈与氯甲酸甲酯的单-N-去甲基化,然后将氨基甲酸酯基团裂解。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可有效保护小鼠免受最大电击(MES)诱发的癫痫发作(剂量为30 mg / kg) 。