钯催化吲哚的 C-2 和 C-3 双重 C-H 功能化：氟化异卡波碱类似物的合成。
Palladium-Catalyzed C-2 and C-3 Dual C-H Functionalization of Indoles: Synthesis of Fluorinated Isocryptolepine Analogues.
机构信息
Tianjin Key Laboratory of Structure and Performance for Functional Molecules, College of Chemistry, Tianjin Normal University, Tianjin 300387, People's Republic of China.
School of Pharmacy, Key Laboratory of Molecular Pharmacology and Drug Evaluation, Ministry of Education, Collaborative Innovation Center of Advanced Drug Delivery System and Biotech Drugs in Universities of Shandong, Yantai University, Shandong, Yantai, 264005, People's Republic of China.
出版信息
Org Lett. 2020 Jun 5;22(11):4097-4102. doi: 10.1021/acs.orglett.0c01159. Epub 2020 May 27.
Here we report a protocol to synthesize diversiform fluorinated isocryptolepine analogues with potential biological activities in one step via directed C-2 and C-3 dual C-H functionalization of indoles. We also attempted to take into account fluorinated imidoyl chlorides as a novel kind of synthons in the directed C-H functionalization reactions. As a result, a variety of fluorinated isocryptolepine analogues were obtained in up to 96% yield. Moreover, we conducted control experiments to disclose the reaction mechanism.
在这里，我们报告了一种通过吲哚的定向 C-2 和 C-3 双重 C-H 官能化一步合成具有潜在生物活性的多样氟化异卡波林类似物的方案。我们还试图考虑将氟化亚氨酰氯作为导向 C-H 官能化反应中的一种新型合成子。结果，以高达 96%的产率获得了多种氟化异卡波林类似物。此外，我们进行了控制实验以揭示反应机制。
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