摘要/Abstract

发展了一种通过铑催化碳氢二氟烯丙基化/N-碘代丁二酰亚胺（NIS）介导的环化反应构建含氟3，4-二氢嘧啶并[1，6-a]吲哚-1（2H）-酮衍生物的方法.该方法具有反应条件温和、底物适用范围广等优点.该方法为构建用于发现药物的含氟杂环化合物提供了潜在的策略.
关键词: 碳氢活化, 氟化学, 铑催化
A mild and facile two-step strategy has been developed for the synthesis of fluorinated 3,4-dihydropyrimido-[1,6-a]-indol-1(2H)-ones through Cp*Rh(III)-catalyzed C-H 3,3-difluoroallylation and N-iodosuccinimide (NIS)-mediated cyclization. This strategy featured broad synthetic generality, unique versatility and high efficiency, which provided a potential tool for the construction of fluorine-containing heterocycles for drug discovery.
Key words: C-H activation, fluorine chemistry, rhodium catalysis


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