摘要
苯并咪唑是一种重要的药用活性中间体,糖基苯并咪唑及其衍生物也有着广泛的药用价值和生物活性,因此对其合成研究具有重要的意义。以空气为氧化剂,在室温条件下,于弱酸性水溶液中,将一系列还原性单糖、二糖与邻苯二胺缩合,以较高收率得到一系列糖基苯并咪唑类化合物,经熔点、红外光谱、核磁等方式进行了结构表征。与传统方法相比,此方法原料易得,反应条件温和,以水为溶剂,为糖基化衍生物的绿色合成提供了依据。
Benzimidazole is an important intermediate of active pharmaceutical. Aldo-benzimidazoles and their deriva- tives have wide pharmaceutical values and biological activities. Therefore, the research on synthesis has an important sig- nificance. Using air as an oxidant in weakly acidic aqueous solution, a series of monosaccharide and disaccharide undergo a direct oxidative condensation reaction with o-phenylenediamine at room temperature to give the aldo-benzimidazole products in high yields. The target products were identified by the melting point, IR, ^1HNMR and 13 CNMR. Compared with the traditional methods, the green method has the advantages of raw material easy to get, mild reaction conditions and water as solvent, which provide evidence for the research of the synthesis of glycosylated derivatives.
出处
《化学试剂》
CAS
CSCD
北大核心
2014年第6期497-499,545,共4页
Chemical Reagents
基金
山东省自然科学基金资助项目(ZR2010CM-037)
农业部科研资助项目(2130108)
关键词
苯并咪唑
还原糖
邻苯二胺
氧化
酰化
aldo-henzimidazoles
reducing sugar
o-phenylenediamine
air
peracetatate synthesis
