Preparation of 5-heteroaryl substituted 1-(4-fluorophenyl)-1H-indoles via palladium-catalyzed Negishi and Stille cross-coupling reactions
Palladium-catalyzed Negishi cross-coupling of 5-1-(4-fluorophenyl)indolylzinc chloride with N-methyl-halopyrazoles, bromopyridines and bromopyrimidines in gram scale gave the corresponding cross-coupled products in 38-85% yield.
The present invention relates to pyridinyloxy- and pyrimidinyloxyindole derivatives, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
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(2008/06/13)
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