高效微波辅助合成6-羟基-2(1H)-喹啉酮  

Highly Efficient Synthesis of 6-Hydroxy-2(1H)-Quinolinone Under Microwave Assistance

作　　者：苏虎[1] 宋秀庆[1] 闫红[1] 

机构地区：[1]北京工业大学生命科学与生物工程学院,北京100022

出　　处：《辽宁石油化工大学学报》2006年第4期51-52,55,共3页Journal of Liaoning Petrochemical University

基　　金：教育部科学技术研究重点项目(03006);北京市教育委员会科技发展面上项目(20051005027)。

摘　　要：6-羟基-2(1H)-喹啉酮(Ⅱ)是治疗充血性心力衰竭(托波利农)、精神失常、血小板聚集、肿瘤、溃疡和过敏等药物的重要中间体,且其衍生物在对HIV-1逆转录酶非核苷抑制剂的设计和改进病毒抗药性方面也起到了重要作用。但现有Ⅱ的合成方法存在反应时间过长,操作复杂等问题。为了改善Ⅱ的合成方法,将微波辅助法引入实验过程。以6-甲氧基喹啉为起始原料,经氧化、重排、脱甲基后,反应时间从原来的54 h缩短到8 h,反应步骤由3步简化为2步,目标化合物的收率也有所提高,从而达到快速、简捷、高效地合成Ⅱ的目的。The compound of 6 - hydroxy - 2（1H） - quinolinone （ Ⅱ ） is important intermediate with treating hyperaemie heart failure （toborinone） and other disease, such as anoia, hemoblast conglomeration, tumour, canker, allergy et al, they also can be designed for anti HIV - 1 non - nueleoside inhibitor of reverse transcriptase. But there were many discommodious faetors to synthesize Ⅱ , the microwave - assisted method was applied to access an efficient way of Ⅱ. The resuits show that the peried of synthesis has been declined from 54 h to 8 h when using 6 methoxyquinoline as raw material. After oxidation, rearrangement and demethylation, the process is simplified by combing three in two. This method is a high efficient and easy way by eliding the most of disposing steps such as neutralisation, extraction, recrystallization during the preparation.

关 键 词：微波 合成 6-羟基-2(1H)-喹啉酮 6-甲氧基喹啉 托波利农 

分 类 号：TQ224.7[化学工程—有机化工]