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Tandem C-N/Suzuki Coupling as the Key Step in the Syntheses of KDR Kinase Inhibitors
Y.-Q. Fang, R. Karisch, M. Lautens*
University of Toronto, Canada
24 April 2007 (online)
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%.