Synthesis of 5-substituted-1H-indol-2-yl-1H-quinolin-2-ones: A novel class of KDR kinase inhibitors

A number of approaches for the synthesis of the 1H-indol-2-yl-1H-quinolin-2-one ring system found in the potent and selective kinase insert domain receptor (KDR) inhibitor are described. The key structural feature of KDR inhibitors is the indol-2-ylquinolin-2-one ring system bearing a substituent in the 5-position of the indole ring.