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Synfacts 2007(5): 0526-0526  
DOI: 10.1055/s-2007-968429
Metal-Mediated Synthesis
© Georg Thieme Verlag Stuttgart · New York

Tandem C-N/Suzuki Coupling as the Key Step in the Syntheses of KDR Kinase Inhibitors

Contributor(s): Paul Knochel, Tobias Thaler
Y.-Q. Fang, R. Karisch, M. Lautens*
University of Toronto, Canada
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Publication History

Publication Date:
24 April 2007 (online)

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Significance

The Pd-catalyzed tandem C-N/Suzuki coupling reaction which offers an easy access to 2-substituted heteroaryl indoles is applied to the syntheses of biologically active KDR kinase inhibitors. The inhibitors can thus be synthesized in only five to seven steps with overall yields up to 63%.