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本文合成了12个3,4-二取代芳脂胺类化合物。其中化合物Ⅰ_(a-e)以取代芳醛与3,4-二取代苯乙胺缩合,还原后成盐;化合物Ⅲa-e以3,4-二取代苯甲醛与相应的胺同法制备;化合物Ⅱa,Ⅱb则分别以Ⅰa和Ⅰe为原料进行氮甲基化和氮磺酰化反应制备。将11个化合物进行实验性大鼠急性降压实验,大部分呈现降压活性,其中N-(4-二甲氨基苄基)-3,4-二甲氧基苯乙胺盐酸盐(Ⅰe),N-甲基-N-(3,4,5-三甲氧基苄基)-3,4-二甲氧基苯乙胺盐酸盐(Ⅱa)和N-(4-甲基苯磺酰基)-N-(4-二甲氨基苄基)-3,4-二甲氧基苯乙胺(Ⅱb)有明显的降压作用,化合物Ⅰe的降压作用尤为显著。
In this paper, 12 3,4-disubstituted arylaliphatic amines were synthesized. Among them, compoundⅠ_ (ae) was condensed with 3,4-disubstituted phenylethylamine and reduced to form salt. CompoundⅢa-e was prepared by the same method as the corresponding amine with 3,4-disubstituted benzaldehyde. CompoundⅡa , Ⅱb, respectively, Ⅰa and Ⅰe as raw materials for nitrogen methylation and sulfonation reaction. Eleven compounds were subjected to an acute antihypertensive experiment in rats, most of which showed antihypertensive activity. Among them, N- (4-dimethylaminobenzyl) -3,4-dimethoxyphenethylamine hydrochloride ), N-methyl-N- (3,4,5-trimethoxybenzyl) -3,4-dimethoxyphenethylamine hydrochloride (IIa) and N- Acyl) -N- (4-dimethylaminobenzyl) -3,4-dimethoxyphenethylamine (IIb) has obvious antihypertensive effect, the compound Ⅰe antihypertensive effect is particularly significant.