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Versatile ligand for palladium-catalyzed meta-C—H functionalizations of aromatic substrates

机译：钯催化芳族底物间位C-H官能化的多功能配体

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摘要

A class of mono-protected 3-amino-2-hydroxypyridine (MPAHP) ligands that enable the meta-C—H arylation of anilines, phenols, phenylacetic acids, and biologically relevant heterocyclic compounds using norbornene as a transient mediator is disclosed, such as in the formation of a reaction product of Formula IA:; embedded image

;The applicability of this meta-arylation methodology in the pharmaceutical industry is illustrated for heteroaryl substrates and heteroaryl iodide coupling partners, a feat made possible by using the MPAHP ligand. The enabling nature of MPAHP ligands to achieve other meta-C—H functionalization processes is also illustrated by the development of a meta-C—H amination reaction and a meta-C—H alkynylation reaction.

机译：公开了一类单保护的3-氨基-2-羟基吡啶（MPAHP）配体，其能够使用降冰片烯作为瞬时介体，使苯胺，苯酚，苯乙酸和生物学相关的杂环化合物进行间位-CH芳基化，例如在形成式IA的反应产物中： “嵌入式图像”

;说明了该杂芳基化方法学在制药工业中对杂芳基底物和杂芳基碘化物偶联伙伴的适用性，这是通过使用MPAHP配体实现的壮举。 MPAHP配体实现其他meta-CH功能化过程的使能性质也通过meta-CH胺化反应和meta-CH烷基化反应的发展得以说明。

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公开/公告号US10696635B2

专利类型
公开/公告日2020-06-30

原文格式PDF
申请/专利权人 THE SCRIPPS RESEARCH INSTITUTE;
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申请/专利号US201716094707
发明设计人 JIN-QUAN YU;
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申请日2017-04-18
分类号C07C6/02;C07D213/68;C07D401/14;C07D405/14;C07D231/12;C07D231/56;C07D401/12;C07D405/12;C07D239/42;C07D409/12;C07D409/14;C07D241/12;C07D413/12;C07D217/12;C07D213/36;C07D213/26;B01J23/44;C07D213/30;C07D213/40;C07D213/55;C07D213/72;C07D215/38;C07D217/18;C07D217/24;C07D239/26;
国家 US
入库时间 2022-08-21 11:30:42

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