Rhodium-catalyzed redox-neutral coupling of phenidones with alkynes
Rhodium-catalyzed redox-neutral coupling of phenidones with alkynes
复制标题
铑催化菲尼酮与炔烃的氧化还原中性偶联
DOI：
10.1039/c7ob01271c
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发表时间：
2017-07-21
影响因子：
3.2
通讯作者：
Zhang, Ao
中科院分区：
文献类型：
--
作者：
Fan, Zhoulong;Lu, Heng;Zhang, Ao
以苯尼酮为原料，经铑催化氧化还原-中性C-H活化，实现了n取代吲哚衍生物的可切换合成。在这个方案中，我们首先披露了Rh（III）催化剂的反应活性可以通过使用醋酸钯作为添加剂来增强。具有代表性的特点是无外部氧化剂，适用于末端炔，反应时间短，操作简单。高效的PARP-1抗癌抑制剂的经济合成进一步证明了这种方法的实用性。
A switchable synthesis of N-substituted indole derivatives from phenidones via rhodium-catalyzed redox-neutral C-H activation has been achieved. In this protocol, we firstly disclosed that the reactivity of Rh(III) catalysis could be enhanced through employing palladium acetate as an additive. Some representative features include external oxidant-free, applicable to terminal alkynes, short reaction time and operational simplicity. The utility of this method is further showcased by the economical synthesis of potent anticancer PARP-1 inhibitors.