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为了寻找外周抗胆碱作用强的托品类药物,合成了山莨菪碱和樟柳碱的类似物(Ⅲ和Ⅳ)、溴甲烷季铵盐(Ⅴ～Ⅷ)和硫酸甲酯季铵盐(Ⅸ和Ⅹ)。在探索向肌性较强的脏器解痉药方面,合成了这两个碱的溴正丁烷季铵盐(Ⅺ和Ⅻ)及氮氧化合物(ⅩⅣ和ⅩⅤ)。化合物(Ⅲ～ⅩⅤ)的物理常数及核磁共振光谱数据分别列于表1和表2。这些化合物的抗胆碱活性筛选结果表明,甲基季铵盐比其母体碱的活性强,其中以山莨菪碱溴甲烷季铵盐的活性最强。
In order to find the peripheral anticholinergic drugs, anophenanthroline and anisodine analogues (Ⅲ and Ⅳ), methyl bromide bromide (Ⅴ ~ Ⅷ) and methyl sulfate quaternary ammonium salt (Ⅸ and Ⅹ). The two alkali brominated n-butane quaternary ammonium salts (Ⅺ and Ⅻ) and the oxynitrides (Ⅹ Ⅹ and ⅩⅤ) were synthesized in order to explore muscular spasm antispasmodics. The physical constants and nuclear magnetic resonance spectrum data of the compounds (III-XV) are shown in Tables 1 and 2, respectively. The results of the anticholinergic screening of these compounds show that methyl quaternary ammonium salt is more active than its parent base and that anisodamine bromide methyl quaternary ammonium salt is the most active.