Asymmetric Dearomatizing Fluoroamidation of Indole Derivatives with Dianionic Phase-Transfer Catalyst
Asymmetric Dearomatizing Fluoroamidation of Indole Derivatives with Dianionic Phase-Transfer Catalyst
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DOI：
10.1021/acs.orglett.0c02026
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发表时间：
2020-07-17
期刊：
影响因子：
5.2
通讯作者：
Hamashima, Yoshitaka
中科院分区：
文献类型：
--
作者：
Egami, Hiromichi;Hotta, Ryo;Hamashima, Yoshitaka
用二元酸盐相转移催化剂研究了吲哚类化合物的不对称脱芳构化氟环化反应。该反应在温和的反应条件下进行，以高度对映选择性的方式提供氟吡咯吲哚衍生物。吲哚环上的各种取代模式具有很好的容忍性。为了促进反应并确保重现性，水的加入是必不可少的，并讨论了其可能的作用。
Asymmetric dearomatizing fluorocyclization of indole derivatives was investigated using a dicarboxylate phase-transfer catalyst. This reaction proceeds under mild reaction conditions to provide fluoropyrroloindoline derivatives in a highly enantioselective manner. Various substitution patterns on the indole ring are well tolerated. To facilitate the reaction and ensure reproducibility, the addition of water is essential, and its possible role is discussed.