摘要
硫醚、亚砜和砜在农药、药物及材料科学上是一类常见且重要的结构单元,因而C-S键的构建是有机化学研究的热点。课题组前期以亚磺酸盐为磺酰化试剂,发展了一类高效的异喹啉酮-C-4位磺酰化反应的方法。本研究在前期工作基础上,以异喹啉酮为底物,芳基亚磺酸为磺酰化试剂,在NaI催化下及空气氧化下发生C-4位C(sp^(3))-H键的直接磺酰化反应,并以中等偏上的收率得到相应的产物。该方法具有一定的底物适用范围,可为相关衍生物的合成提供方法参考。
The sulfur ether,sulfoxide and sulfone skeletons are important structural building blocks that are prevalent in various agrochemicals,pharmaceuticals and materials science.Thus,the formation of C-S bond is always a research hotspot in organic chemistry.Sulfinates were used as the sulfonylating agents enabled a highly efficient method for the preparation of C-4 sulfonylated isoquinolinones.Isoquinolinones were taken as substrates and aryl sulfinic acids were used as sulfonylating agents,the direct C(sp^(3))-H bond sulfonylation of isoquinolinones on the C-4 position was realized under NaI catalyzed conditions in AcOH/DMSO,and the corresponding products were obtained in moderate to good yields.The disclosed procedure tolerated a certain substrate scope and can be used in the preparation C-4 sulfonylated isoquinolinone derivatives.
作者
王丽丽
韦邦花
程飞
毛远湖
张吉泉
WANG Li-li;WEI Bang-hua;CHENG Fei;MAO Yuan-hu;ZHANG Ji-quan(School of Medicine and Health Management,Guizhou Medical University,Guizhou Guiyang 550025;School of Pharmacy,Guizhou Medical University,Guizhou Guiyang 550025;Guizhou Provincial Engineering Technology Research Center for Chemical Drug R&D,Guizhou Medical University,Guizhou Guiyang 550025,China)
出处
《广州化工》
CAS
2021年第14期34-36,54,共4页
GuangZhou Chemical Industry
基金
贵州省自然科学基金重点项目(黔科合基础[2020]1Z073)
贵州省卫生计生委科学技术基金项目(gzwjkj2019-1-179)
贵州省高等学校大学生创新训练计划项目(20195200128)。
关键词
C-S键
异喹啉酮
磺酰化
催化
C-S bond
isoquinolinone
sulfonylation
catalyzation
