Au-Catalyzed Cross-Coupling of Arenes via Double C-H Activation
The first methodology for Au(I/III)-catalyzed oxidative cross-coupling of arenes via double C-H activation has been developed. The reaction is fully selective for the cross-coupling between electron-rich hetero-/carbocyclic arenes and electron-poor arenes bearing relatively acidic C-H bonds. The inherently high cross-selectivity of the system obviates the need for directing groups or a large excess of one of the coupling partners.
Cambeiro, Xacobe C.,Ahlsten, Nanna,Larrosa, Igor
supporting information
p. 15636 - 15639
(2016/01/09)
A closer look at the bromine-lithium exchange with tert-butyllithium in an aryl sulfonamide synthesis
A practical protocol for the one-pot synthesis of various aryl sulfonamides, notably of pyridine-core-substituted 7-azaindolyl sulfonamides, is described. A key step is the well-known bromine-lithium exchange reaction of an aryl bromide with tert-butyllithium (t-BuLi). Differing from the common practice to use 2 or more equiv of organolithium, the exact amount of t-BuLi needed for a sufficient exchange reaction is determined for each aryl bromide in a GC-MS-assisted experiment.
Waldmann, Christopher,Schober, Otmar,Haufe, Guenter,Kopka, Klaus
p. 2954 - 2957
(2013/07/26)
AZAINDOLES USEFUL AS INHIBITORS OF ROCK AND OTHER PROTEIN KINASES
The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
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Page/Page column 180-189
(2008/06/13)
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