【摘要】 报道了7个2-烷胺乙酰和2-烷胺乙基-1-对甲苯基四氢异喹啉衍生物的合成。在制备1-对甲苯基-3,4-二氢异喹啉中,改进反应条件,P₂O₅用量由原来1∶5mol减少到1∶1.1mol,收率不受影响,简化后处理操作。化合物经乌头碱致大鼠心律失常模型初步试验结果,均具有抗心律失常活性,其中化合物Ⅱa-2的抗室性心律失常作用和对心脏毒性优于安搏律定。更多还原

【Abstract】 Seven 2-alkylaminoacetyl-and 2-alkylaminoethyl-1-p-methylphenyltetrahy-droisoquinoline derivatives were synthesized from N-phenethyl-p-methylbenzamide by the Bisohler-Napieralski reaction, reduction with KBH4, chloroaoetylation, amination and others. Their antiarrhythmio activities were assessed. All of these compounds exhibited antiarrhythmio effects against aoonitine arrhythmia in rats. The compound IIa-2 had higher antiarrhythmio potency, a weaker oardiotoxio effect and lower acute toxioity than Aprindine.更多还原