Ligand-Promoted meta-C-H Amination and Alkynylation.

Ligand-Promoted meta-C-H Amination and Alkynylation.
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DOI:
10.1021/jacs.6b08942
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发表时间:
2016-10-26
影响因子:
15
通讯作者:
Yu JQ
Yu JQ
中科院分区:
化学1区
文献类型:
--
作者:
Wang P;Li GC;Jain P;Farmer ME;He J;Shen PX;Yu JQ

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Meta-C–H amination and meta-C–H alkynylation of aniline and phenol substrates using a modified norbornene (methyl bicyclo[2.2.1]hept-2-ene-2-carboxylate) as a transient mediator has been developed for the first time. Both the identification of a mono-protected 3-amino-2-hydroxypyridine/pyridone type ligand and the use of a modified norbornene as a mediator are crucial for the realization of these two unprecedented meta-C–H transformations. A variety of substrates are compatible with both meta-C–H amination and meta-C–H alkynylation. Amination and alkynylation of heterocyclic substrates including indole, indoline, and indazole afford the desired products in moderate to high yields.
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