9-咔唑-羧酸化合物的微波合成及其生物活性研究

9-咔唑 -羧酸化合物不但是医药1] 、有机光导材料2 ] 的中间体 ,而且其本身亦具有干扰素诱导能力3] .近年来 ,我们4 ] 应用 9-咔唑 -乙酸和丙酸作为高效液相色谱分析氨基酸、胺和醇类的衍生化试剂 .目前所合成的此类化合物很少 .近 1 5年以来 ,微波在有机合成中的应用已发展成为一个新的研究领域5] ,许多反应已在微波炉中高产率快速地实现了 .本文采用微波辐照法快速合成了系列 9-咔唑 -羧酸化合物 3 a— 3 m,优化了反应条件 ,并测试了它们的生物活性 .反应式如下 :丷4R5丯HR3 R2R1( 1) +Br R6COOC2 H5( 2 ) 丷4R5丯R6COOHR3 R…

Studies on the Synthesis,Properties and Biological Activities of (9-Carbazoly)-carboxylic Acids

This paper investigated a rapid one pot synthesis method of some substituted(9 carbazoly) carboxylic acids(3a_3m). The reaction was carried out by mixing of the 9H carbazoles derivatives with bromo esters and potassium hydroxide using DMF as solvent under microwave irradiation without catalyst. The optimized experiment conditions were 4_8 min irradiation time and 375 W microwave power. The required range of molar ratio of KOH to substituted carbazole was 3_5. The biological activities of some compounds have been tested. They have medium to weak antimicrobial activities.