叔丁基过氧化氢介导的 3-芳磺酰基喹啉的串联合成。
tert-Butyl Hydroperoxide Mediated Cascade Synthesis of 3-Arylsulfonylquinolines.
机构信息
Department of Chemistry, College of Chemistry and Chemical Engineering, and the Key Laboratory for Chemical Biology of Fujian Province, Xiamen University , Xiamen 361005, China.
Key Laboratory of Bioorganic Phosphorus Chemistry and Chemical Biology (Ministry of Education), Department of Chemistry, Tsinghua University , Beijing 100084, China.
出版信息
Org Lett. 2016 Mar 18;18(6):1286-9. doi: 10.1021/acs.orglett.6b00198. Epub 2016 Mar 9.
3-Arylsulfonylquinoline derivatives play important roles as pharmaceutical drugs. A new method for the synthesis of 3-arylsulfonylquinoline derivatives has been achieved through tert-butyl hydroperoxide mediated cycloaddition between N-propargyl aromatic amine derivatives and arylsulfonylhydrazides without the addition of any metals. This transformation offers a straightforward route to the formation of a C-S bond and quinoline ring in one step via a sulfonylation-cyclization-aromatization process.
3-芳基磺酰基喹啉衍生物在药物方面起着重要的作用。通过 N-丙炔基芳胺衍生物和芳基磺酰基腙之间在叔丁基过氧化氢介导下的环加成反应，无需添加任何金属，实现了一种新的 3-芳基磺酰基喹啉衍生物的合成方法。该转化通过磺酰化-环化-芳构化过程一步形成 C-S 键和喹啉环，提供了一条直接的途径。
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