- One-pot ortho-amination of aryl C-H bonds using consecutive iron and copper catalysis
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A one-pot approach for ortho-coupling of arenes with non-actived N-nucleophiles has been developed using sequential iron and copper catalysis. Regioselective ortho-activation of anisoles, anilines and phenols was achieved through iron(iii) triflimide catalysed iodination, followed by a copper(i)-catalysed, ligand-assisted coupling reaction with N-heterocycle, amide and sulfonamide-based nucleophiles. The synthetic utility of this one-pot, two-step method for the direct amination of ortho-aryl C-H bonds was demonstrated with the late-stage functionalisation of 3,4-dihydroquinolin-2-ones. This allowed the preparation of a TRIM24 bromodomain inhibitor and a series of novel analogues.
- Henry, Martyn C.,McGrory, Rochelle,Faggyas, Réka J.,Mostafa, Mohamed A. B.,Sutherland, Andrew
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p. 4629 - 4639
(2019/05/17)
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- Palladium-catalyzed ortho-alkoxylation of anilides via C-H activation
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A palladium-catalyzed ortho-alkoxylation of anilides with both primary and secondary alcohols via ligand-directed C-H activation has been explored. This alkoxylation promoted by catalytic methanesulfonic acid proceeds well at room temperature in most cases and affords aryl alkyl ethers in moderate to good yields.
- Jiang, Tao-Shan,Wang, Guan-Wu
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p. 9504 - 9509,6
(2012/12/12)
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