为寻找新的高活性哌嗪类化合物,根据药物拼合原理,试验设计合成了6个未见报道的哌嗪系列化合物(3a-f)。以哌嗪为起始原料,通过与取代苄氯反应得到1-(取代苄基)哌嗪1,1与苯甲酸-2-氯乙酯得到目标化合物(3a-f)。结果表明:改进了中间体1的...为寻找新的高活性哌嗪类化合物,根据药物拼合原理,试验设计合成了6个未见报道的哌嗪系列化合物(3a-f)。以哌嗪为起始原料,通过与取代苄氯反应得到1-(取代苄基)哌嗪1,1与苯甲酸-2-氯乙酯得到目标化合物(3a-f)。结果表明:改进了中间体1的制备方法,使用了异丙醇和水作为混合溶剂,实现了温和的反应条件,产率达到70%以上。结论:所有的化合物经IR、1 H NMR、MS及元素分析表征,证明了合成方法的可靠性。展开更多
Four benzyl substituted pyridine bromide quaternary ammonium salts,1-benzyl-2′-methylpyridinium bromide([Bz-2-CH3Py]Br),1-benzyl-4′-methylpyridinium bromide([Bz-4-CH3Py]Br),1-benzyl-4′-aminopyridinium bromide([Bz-4...Four benzyl substituted pyridine bromide quaternary ammonium salts,1-benzyl-2′-methylpyridinium bromide([Bz-2-CH3Py]Br),1-benzyl-4′-methylpyridinium bromide([Bz-4-CH3Py]Br),1-benzyl-4′-aminopyridinium bromide([Bz-4-NH2Py]Br) and 1-benzyl-4′-dimethylaminopyridinium bromide([BzDMAP]Br),were synthesized by the reaction of benzyl bromide and 2-methylpyridine,4-methylpyridine,4-aminopyridine or 4-dimethylaminopyridine.Their components and structures were characterized by elemental analyses,infrared spectra,electronic spray mass spectra and conductivity.The experimental results of antibacterial activities indicated that the four salts exhibited good antibacterial properties for colibacillus,bacillus subtilus,aurococcus and bacillus thuringiensis.展开更多
文摘为寻找新的高活性哌嗪类化合物,根据药物拼合原理,试验设计合成了6个未见报道的哌嗪系列化合物(3a-f)。以哌嗪为起始原料,通过与取代苄氯反应得到1-(取代苄基)哌嗪1,1与苯甲酸-2-氯乙酯得到目标化合物(3a-f)。结果表明:改进了中间体1的制备方法,使用了异丙醇和水作为混合溶剂,实现了温和的反应条件,产率达到70%以上。结论:所有的化合物经IR、1 H NMR、MS及元素分析表征,证明了合成方法的可靠性。
文摘Four benzyl substituted pyridine bromide quaternary ammonium salts,1-benzyl-2′-methylpyridinium bromide([Bz-2-CH3Py]Br),1-benzyl-4′-methylpyridinium bromide([Bz-4-CH3Py]Br),1-benzyl-4′-aminopyridinium bromide([Bz-4-NH2Py]Br) and 1-benzyl-4′-dimethylaminopyridinium bromide([BzDMAP]Br),were synthesized by the reaction of benzyl bromide and 2-methylpyridine,4-methylpyridine,4-aminopyridine or 4-dimethylaminopyridine.Their components and structures were characterized by elemental analyses,infrared spectra,electronic spray mass spectra and conductivity.The experimental results of antibacterial activities indicated that the four salts exhibited good antibacterial properties for colibacillus,bacillus subtilus,aurococcus and bacillus thuringiensis.
