摘要
硝基吡啶类化合物广泛用于有机合成,特别是杂环药物及细胞因子抑制剂的合成。以粘溴酸为原料,分别经与亚硝酸钠反应、与3-氨基巴豆酸乙酯环合、水解,与DPPA反应、脱保护等五步反应最终得到目标产物2-甲基-3-氨基-5-硝基吡啶。此方法仅需要最后一步进行柱纯化,操作简单,后处理方便,总收率为9.1%。
Nitropyridine compound is widely used in organic synthesis,especially in heterocyclic drugs and cytokine inhibitors.Mucobromic acid as raw material is chosed,achieved the target compound in five steps which are respectively reaction with sodium nitrite,cyclization,hydrolysis,reaction with DPPA and deprotection.The method is simple.The total yield is 9.1%.
出处
《科学技术与工程》
2011年第8期1841-1843,共3页
Science Technology and Engineering
