一些新型生物活性1,3,4-恶二唑基硝基吲哚的合成以及硝基吲哚-2-羧酸乙酯的改进费歇尔吲哚合成法。
Synthesis of some new biologically active 1,3,4-oxadiazolyl nitroindoles and a modified Fischer indole synthesis of ethyl nitro indole-2-carboxylates.
作者信息
Narayana B, Ashalatha B V, Vijaya Raj K K, Fernandes J, Sarojini B K
机构信息
Department of Post-Graduate Studies and Research in Chemistry, Mangalore University, Mangalagangotri 574 199, India.
出版信息
Bioorg Med Chem. 2005 Aug 1;13(15):4638-44. doi: 10.1016/j.bmc.2005.04.068.
An efficient and modified synthesis of ethyl-4-nitro/5-nitro/6-nitro and 7-nitroindole-2-carboxylates is described. Carbohydrazides of corresponding ethyl nitroindole-2-carboxylates underwent smooth one-step transformation to 1,3,4-oxadiazolyl nitroindoles (4a-l) on reaction with aromatic carboxylic acids in the presence of phosphorus oxychloride. An alternate method to synthesize 1,3,4-oxadiazolyl nitroindoles is also described. Among the newly synthesized 1,3,4-oxadiazolyl nitroindoles, a few compounds are studied for anti-inflammatory activity.
描述了一种高效且经过改进的4-硝基/5-硝基/6-硝基和7-硝基吲哚-2-羧酸乙酯的合成方法。相应的硝基吲哚-2-羧酸乙酯的酰肼在三氯氧磷存在下与芳香羧酸反应时，顺利地一步转化为1,3,4-恶二唑基硝基吲哚（4a - l）。还描述了一种合成1,3,4-恶二唑基硝基吲哚的替代方法。在新合成的1,3,4-恶二唑基硝基吲哚中，对一些化合物进行了抗炎活性研究。
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