摘要
丙二酸二乙酯在醇溶液中,与氢氧化钾皂化得到丙二酸单乙酯钾盐,然后在N,N'-羰基二咪唑(CDI)作用下,与2-硝基苯乙酸进行亲核加成得到4-(2-硝基苯基)-乙酰乙酸乙酯,再经三氯化钛的催化还原环化制得医药中间体2-吲哚乙酸乙酯,收率达72.2%。
2- indole acetic acid ethyl ester, the important drug intermediate, was synthesized from diethyl malonate by saponification reaction with potassium hydroxide in the presence of alcohol solution to give ethyl malonate potassium salt and nucleophilic addition with 2-nitrophenyl acetic acid to give 4-(2-nitrophenyl)-ethylacetoacetate using N,N'-carbonyldiimidazole(CDl), and then reduct cyclization reaction upon the catalysis of titanium trichloride with an overall yield of about 72.2%.
出处
《武汉纺织大学学报》
2015年第3期63-66,共4页
Journal of Wuhan Textile University
基金
湖北省教育厅科学技术研究项目(B20129202)
关键词
2-吲哚乙酸乙酯
医药中间体
合成
2- indole acetic acid ethyl ester
pharmaceutical intermediates
synthesis