期刊
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
卷 131, 期 9, 页码 3291-3306出版社
AMER CHEMICAL SOC
DOI: 10.1021/ja808332k
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资金
- NSERC
- Research Corporation
- Sloan Foundation
- ACS
- Merck Frosst
- Merck Inc.,
- Amgen
- Eli Lilly
- Astra Zeneca
- Boehringer Ingelheim
Palladium-catalyzed direct arylation reactions are described with a broad range of azine and azole N-oxides. In addition to aspects of functional group compatibility, issues of regioselectivity have been explored when nonsymmetrical azine N-oxides are used. In these cases, both the choice of ligand and the nature of the azine substituents play important roles in determining the regioisomeric distribution. When azole N-oxides are employed, preferential reaction is observed for arylation at C2 which occurs under very mild conditions. Subsequent reactions are observed to occur at C5 followed by arylation at C4. The potential utility of this methodology is illustrated by its use in the synthesis of a potent sodium channel inhibitor 1 and a Tie2 Tyrosine Kinase inhibitor 2.
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