Huang Kuo-Ting, Sun Chung-Ming
Department of Chemistry, National Dong Hwa University, Shou-Feng, Hualien 974, Taiwan.
Bioorg Med Chem Lett. 2002 Apr 8;12(7):1001-3. doi: 10.1016/s0960-894x(02)00091-4.
Liquid-phase synthesis of 2-arylaminobenzimidazoles using soluble polymer support strategy is first described. The key step to benzimidazole skeleton is achieved in the presence of diisopropylcarbodimide (DICDI) and isothiocyanates. A mechanism study for one-pot cyclodesulfurization is also investigated on the support. A wide range of benzimidazole derivatives is synthesized in excellent yield and purity just by simple wash and precipitation.
首次描述了使用可溶性聚合物载体策略进行2-芳基氨基苯并咪唑的液相合成。在二异丙基碳二亚胺(DICDI)和异硫氰酸酯存在下实现了苯并咪唑骨架的关键步骤。还在载体上研究了一锅法环脱硫的机理。仅通过简单的洗涤和沉淀就以优异的产率和纯度合成了多种苯并咪唑衍生物。