The three isomeric pivaloylaminopyridines were lithiated in more than 80% yields. Aminopyridine derivatives were treated by 2.5-3 equivalents of the complex BuLi-TMEDA at −10° in diethyl ether. Reaction of the lithiated species with various electrophiles afforded a number of ortho-substituted pivaloylaminopyridines in good yields. Secondary pyridine alcohols were oxidized to the corresponding aminopyridyl
将三种异构体新戊酰
氨基吡啶以超过80%的产率进行
锂化。在
乙醚中,在-10°下用2.5-3当量的复合BuLi-TME
DA处理
氨基
吡啶衍生物。
锂化物种与各种亲电试剂的反应以良好的产率提供了许多邻位取代的新戊酰
氨基吡啶。仲
吡啶醇被氧化成相应的
氨基吡啶基酮。已合成了
吡啶并
嘧啶,苯并
萘啶以及天然抗肿瘤
生物碱玫瑰树碱的类似物,显示了该方法的多功能性。