- Palladium-Catalyzed Regioselective Arylation of Pyrazolo[1,5-a]pyridines via C-H Activation and Synthetic Applications on P38 Kinase Inhibitors
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A direct arylation of pyrazolo[1,5-a]pyridines with aryl iodides selectively occurring at the C-3 and C-7 positions via palladium-catalyzed C-H activation is described. In these reactions, (a) cesium(I) fluoride and (b) silver(I) carbonate were employed a
- Wu, Hung-Chou,Chu, Jean-Ho,Li, Chin-Wei,Hwang, Long-Chih,Wu, Ming-Jung
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p. 288 - 300
(2016/02/05)
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- Optimized scale up of 3-pyrimidinylpyrazolo[1,5-a]pyridine via Suzuki coupling; A general method of accessing a range of 3-(hetero)arylpyrazolo[1,5-a] pyridines
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We have developed an improved synthesis of 3-(hetero)aryl pyrazolo[1,5-a]pyridines (such as 3-(2,5-dichloropyrimidin-4-yl)pyrazolo[1,5-a] pyridine (8)) via an optimized synthesis and Suzuki coupling of 3-pyrazolo[1,5-a]pyridine boronic ester 10. These conditions are applicable to both high throughput chemistry and large scale synthesis of these medicinally important compounds. The scope of this chemistry has been further extended to include the synthesis and coupling of a novel boronic ester, 3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-6,7-dihydro-5H-pyrazolo[5,1-b] [1,3]oxazine (43).
- Bethel, Paul A.,Campbell, Andrew D.,Goldberg, Frederick W.,Kemmitt, Paul D.,Lamont, Gillian M.,Suleman, Abid
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p. 5434 - 5444
(2012/09/08)
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