4-芳环及芳杂环胺甲基酚类化合物的合成

SYNTHESIS OF 4-ARYL/HETERAYLAMINOMETHYL-PHENOLS

摘要: 为了寻找新的抗心律失常药物,本文根据常咯啉部分结构特征,设计并合成了24个4-芳环及芳杂环胺甲基酚类化合物。对其中大部分化合物进行了抗心律失常和抗胆碱动物试验,发现四个化合物:4′-甲氧基-4-羟基-3,5-双吡咯烷甲基-联苯(Ⅳ_(12)),4-(2-噻吩甲酰基)-3,5-双吡咯烷甲基-苯酚盐酸盐(Ⅸ_1),4-(1-咪唑)-3,5-双吡咯烷甲基-苯酚盐酸盐(Ⅸ_3)4-苄基-2-1-(4甲基-哌嗪)甲基-苯酚盐酸盐(Ⅸ_4),其抗心律失常活性均强于常咯啉。

Abstract: On the basis of the partial structural features of Changrolin, twenty four 4-aryl/heterayl-aminomethyl-phenols were designed and then synthesized so as to find new antiarrhythmic agents. The reaction of the substituted phenols with secondary amines and fo