Fang Zaixiang, Wang Yi, Wang Yuanhua
College of Chemistry , Sichuan University , Chengdu 610064 , P.R. China.
Org Lett. 2019 Jan 18;21(2):434-438. doi: 10.1021/acs.orglett.8b03614. Epub 2019 Jan 7.
An efficient Rh(II,II)-catalyzed reaction has been developed under mild conditions. This synthetic method proceeds through iodination/oxidation of readily available isoquinolinium iodide salts under aerobic conditions with good to excellent yields. 4-Iodoisoquinolin-1(2 H)-ones are important building blocks for biologically and medicinally important compounds. The developed methodology was applied to the gram-scale synthesis of a key intermediate in the synthesis of the CRTH2 antagonist CRA-680.
已开发出一种在温和条件下高效的铑（II,II）催化反应。这种合成方法是通过在有氧条件下对易于获得的异喹啉碘盐进行碘化/氧化反应，产率良好至优异。4-碘异喹啉-1(2H)-酮是生物和医学上重要化合物的重要构建模块。所开发的方法应用于CRTH2拮抗剂CRA-680合成中关键中间体的克级规模合成。
