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双齿配体促进的甲醇 C(sp)-H 单芳基化反应。

C(sp)-H Monoarylation of Methanol Enabled by a Bidentate Auxiliary.

机构信息

School of Chemistry and Chemical Engineering, Yangtze Normal University, Chongqing 408100 China.

Key Laboratory of Jiangxi University for Applied Chemistry and Chemical Biology, Yichun University, Yichun 336000, China.

出版信息

Org Lett. 2021 Jan 1;23(1):118-123. doi: 10.1021/acs.orglett.0c03786. Epub 2020 Dec 22.

Abstract

With the assistance of a practical directing group (COAQ), the first catalytic protocol for the palladium-catalyzed C(sp)-H monoarylation of methanol has been developed, offering an invaluable synthesis means to establish extensive derivatives of crucial arylmethanol functional fragments. Furthermore, the gram-scale reaction, broad substrate scope, excellent functional group compatibility, and even the practical synthesis of medicines further demonstrate the usefulness of this strategy.

摘要

在实用导向小组(COAQ)的协助下,首次开发出钯催化的甲醇 C(sp)-H 单芳基化的催化协议,为建立关键芳基甲醇功能片段的广泛衍生物提供了宝贵的合成手段。此外,克级规模的反应、广泛的底物范围、优异的官能团兼容性,甚至是药物的实际合成进一步证明了该策略的有用性。

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