【摘要】 以2,4-二硝基氯苯和乙酰乙酸乙酯为原料,经过亲核置换、还原-环化协同反应,合成了6-氨基-2-甲基吲哚-3-羧酸乙酯,而后在催化剂作用下,与乙酰乙酸乙酯反应生成烯胺,环化合成9-羟基-2,7-二甲基吡咯(2,3-f)喹啉-3-羧酸乙酯;类似地,合成了6-氨基-2-苯基吲哚-3-羧酸乙酯和6-氨基-2-(呋喃-2’-基)吲哚-3-羧酸乙酯.其结构均由1HNMR,IR以及MS波谱数据表征.所得化合物具有抑制肺癌A549细胞生长的活性,其抑制效果具有浓度依赖性.更多还原

【Abstract】 Ethyl 6-amino-2-substituent-indole-3-carboxylate was synthesized via SNAr reaction, reduction and tandem cyclization from 2,4-dinitrochlorobenzene and ethyl acetoacetate. The reaction of ethyl 6-amino-2-methylindole-3-carboxylate with ethyl acetoacetate in the presence of catalyst gave an enamine compound, and then ethyl 9-hydroxy-2,7-dimethylpyrrolo(2,3-f)quinoline-3-carboxylate was obtained by cyclization. Similarly, ethyl 6-amino-2-phenylindole-3-carboxylate and ethyl 6-amino-2-fur-2’-ylindole-3- carboxylate were synthesized. The structures of compounds were determined by 1H NMR, IR and MS spec- tra. These compounds were assayed with inhibitory activity against lung cancer A549 cell growth, and the inhibitory effect on the cell viability was dose-dependent.更多还原