摘要
3-砜基喹啉广泛存在于多种生物活性分子和合成药物中.报道了一种温和条件下,以N-炔丙基苯胺和磺酰氯为原料,通过一锅法连续肼化/砜化/环化反应高效构建3-砜基喹啉类化合物的方法.该方法不仅可以进行克级合成,还可用于药物分子砜基衍生物的合成.
3-Sulfonylquinolines broadly exist in plenty of bioactive molecules and synthetic pharmaceuticals.Herein,an efficient and facile method for direct synthesizing various 3-sulfonylquinolines through one-pot sequential hydrazination/sulfonylation/cyclization reaction from N-propargylanilines and sulfonyl chlorides under mild reaction conditions is reported.This procedure not only can be performed on a gram scale but also be applicable to prepare marketed pharmaceutical derivative.
作者
王苛莉
黄静
刘伟
伍智林
于贤勇
蒋俊
何卫民
Wang Keli;Huang Jing;Liu Wei;Wu Zhilin;Yu Xianyong;Jiang Jun;He Weimin(School of Chemistry and Chemical Engineering,University of South China,Hengyang,Hunan 421001;Key Laboratory of Theoretical Organic Chemistry and Functional Molecule of Ministry of Education,Hunan University of Science and Technology,Xiangtan,Hunan 411201)
出处
《有机化学》
SCIE
CAS
CSCD
北大核心
2022年第8期2527-2534,共8页
Chinese Journal of Organic Chemistry
基金
湖南省教育厅科学研究项目(No.19C0783)
湖南省科技创新计划项目(No.2021RC5028)资助项目。
关键词
3-砜基喹啉
N-炔丙基苯胺
磺酰氯
一锅法
环化反应
3-sulfonylquinolines
N-propargylanilines
sulfonyl chlorides
one pot
cyclization reaction
