3‑Amino-1-methyl‑1H‑pyridin-2-one-Directed PdII Catalysis: C(sp3)–H Activated Diverse Arylation Reaction

Organic Letters(2018)

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摘要
A new bidentate directing group, 3-amino-1-methyl-1H-pyridin-2-one, is introduced to achieve a powerful PdII metallacycle for selective γ-C­(sp3)–H activation and arylation of aromatic and aliphatic carboxylic acid derivatives. The versatility of the directing group is validated for remote arylation of β-C­(sp3)–H, β-C­(sp2)–H, and γ-C­(sp2)–H to achieve therapeutically important 2-pyridone analogues and arylated acid synthons. The traceless removal of the directing group to retrieve the directing element and carboxylic acids makes this method more interesting.
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