医薬品原料としてのサフロールの利用研究 (第1報)

1-アミノアルキルイソキノリン類の合成

抄録

1) 1-Dialkylaminomethyl-3-methyl-6, 7-methylenedioxyisoquinoline (I), bis-(3-methyl-6, 7-methylenedioxy-isoquinolyl (1)-methyl)-alkylamine (II) and tri-(3-methyl-6, 7-methylenedioxy-isoquinolyl (1)-methyl)-amine (III) were prepared by treating 1-chloromethyl-3-methyl-6, 7-methylenedioxyisoquinoline with R₂NH, RNH₂ and NH₃.
2) 1-β-Dialkylaminoethyl-3-methyl-6, 7-methylenedioxyisoquinoline (IV) and bis-(3-methyl-6, 7-methylenedioxyisoquinolyl (1)-ethyl)-alkylamine (V) were obtained by treating β-bromopropionic α′-methyl-β′methoxy-β′-(3, 4-methylenedioxyphenyl)-ethylamide with R₂NH and RNH₂ (R=CH₃ and C₂H₅) and then cyclizing these products.
3) Physiological tests of these compounds showed that antispasmodic action of (II) and (V) was approximately equal to that of papaverine used as a control.