Journal
SYNTHESIS-STUTTGART
Volume 49, Issue 21, Pages 4745-4752Publisher
GEORG THIEME VERLAG KG
DOI: 10.1055/s-0036-1588735
Keywords
borylation; C-H functionalization; iridium; 2-pyridones; site selectivity
Categories
Funding
- JSPS [JP 15K13696, JP 15H05485, JP 24225002]
- Grants-in-Aid for Scientific Research [15H05485, 15K13696] Funding Source: KAKEN
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An iridium-catalyzed site-selective C-H borylation of 2-pyridones has been developed. The site selectivity is predominantly controlled by steric factors, and we can access C4, C5, and C6 C-H on the 2-pyridone ring by the judicious choice of ligand and solvent. Subsequent Suzuki-Miyaura cross-coupling of the borylated products also proceeds to form the corresponding arylated pyridones in good overall yields.
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