3-[(1-甲基-1H-吡咯-2-基)亚甲基]吲哚啉-2-酮的合成研究  

Synthesis of 3-((1-Methyl-1H-pyrrol-2-yl)methylene)indolin-2-one

作　　者：郑静静 广海东 陈莉莉 王永亮 门靖 ZHENG Jing-jing;GUANG Hai-dong;CHEN Li-li;WANG Yong-liang;MEN Jing(Jiangsu Chengkai Traditional Chinese Medicine Co.,Ltd.,Huai’an 211600,China;Hanzhong Branch of Shaanxi Provincial Drug and Vaccine Inspection Center,Hanzhong 723000,China;Shaanxi Dahe Pharmaceutical Co.,Ltd.,Xi’an 710200,China;Xi’an Wanlong Pharmaceutical Co.,Ltd.,Xi’an 710119,China)

机构地区：[1]江苏承开中药有限公司,江苏淮安211600 [2]陕西省药品和疫苗检查中心汉中分中心,陕西汉中723000 [3]陕西大河药业有限责任公司,陕西西安710200 [4]西安万隆制药股份有限公司,陕西西安710119

出　　处：《精细化工中间体》2024年第1期46-48,69,共4页Fine Chemical Intermediates

摘　　要：以吲哚啉-2-酮和N-甲基-2-吡咯甲醛为起始原料,经Aldol缩合反应合成得到3-[(1-甲基-1H-吡咯-2-基)亚甲基]吲哚啉-2-酮。产物结构经核磁共振氢谱(1H NMR)和质谱(ESI-MS)确证,Aldol缩合反应的优化条件为:哌啶作为有机碱催化剂、物料比n(哌啶)∶n(N-甲基-2-吡咯甲醛)∶n(吲哚啉-2-酮)=0.2∶1.2∶1.0、反应溶剂为乙醇、反应温度80℃、反应时间5 h,优化条件下,产物收率达73.4%(以吲哚啉-2-酮计)。3-((1-Methyl-1H-pyrrol-2-yl)methylene)indolin-2-one was synthesized from indoline-2-one and Nmethyl-2-pyrrole-formaldehyde via Aldol condensation reaction.The structure of the product was characterized by proton NMR(1 H NMR)and mass spectrometry(ESI-MS).The optimum conditions of the aldol condensation reaction were as follows:piperidine was used as the organic base catalyst;the molar ratio of materials was n(piperidine)∶n(N-methyl-2-pyrrole-formaldehyde)∶n(indoline-2-one)=0.2∶1.2∶1.0,the reaction solvent was ethanol,the reaction temperature was 80℃,and the reaction time was 5 h.A yield of product was up to 73.4%under these reaction conditions.

关 键 词：吲哚衍生物 舒尼替尼 ALDOL缩合反应 

分 类 号：R97[医药卫生—药品]