高效合成活性吡啶并[4,3,2-de]吡咯并[2,1-b]喹唑啉衍生物  

Efficient Synthesis of Active Pyrido[4,3,2-de]pyrrolo[2,1-b]quinazoline Derivatives

作　　者：付林[1] 王嘉翊 袁月飞 赵成安[1] 陈康杰 和平[2] FU Lin;WANG Jia-yi;YUAN Yue-fei;ZHAO Cheng-an;CHEN Kang-jie;HE Ping(Huazhong Pharmaceutical Company Limited,Hubei Xiangyang 441023;College of Chemical Engineering Hubei University of Arts and Science,Hubei Xiangyang 441053,China)

机构地区：[1]华中药业股份有限公司,湖北襄阳441023 [2]湖北文理学院化学工程学院,湖北襄阳441053

出　　处：《广州化工》2021年第15期30-31,61,共3页GuangZhou Chemical Industry

基　　金：湖北省教育厅科学研究计划项目(D20182602);湖北文理学院大学生创新训练项目(No:S2020105109018);襄阳市软科学研究计划项目。

摘　　要：以间硝基苯胺、N-乙烯基吡咯烷酮、各类醛为起始原料,经由氮杂狄尔斯-阿尔德反应、还原、缩合及氧化芳构化过程高效制备标题化合物,该合成路径无需分离氮杂狄尔斯-阿尔德反应的各立体异构体,具有操作方便、条件简单、收率较高等优点,可以快速构建吡啶并[4,3,2-de]吡咯并[2,1-b]喹唑啉化合物库,为该类化合物的活性筛选提供了基础。目标产物经过了1H NMR、^(13)C NMR、IR和MS表征确认。m-Nitroaniline,N-vinylpyrrolidone and various aldehydes were used as starting materials to efficiently prepare the title compound through aza-Diels-Alder reaction/reduction/condensation and oxidative-aromatization.The synthetic route did not need to separate the diastereoisomer compounds of aza-Diels-Alder reaction.The process had the advantages of convenient operation,simple conditions and high yield,and can be used to construct the library of pyrido[4,3,2-de]pyrrolo[2,1-b]quinazoline compounds quickly,which provided a basis for screening the activity of these compounds.And all the target products were characterized by 1H NMR,^(13)C NMR,IR and HRMS.

关 键 词：合成 氮杂狄尔斯-阿尔德反应 吡啶并[4 3 2-de]吡咯并[2 1-b]喹唑啉 衍生物 芳构化 

分 类 号：TQ463.5[化学工程—制药化工]