A Concise Synthesis of a Novel Antiangiogenic Tyrosine Kinase Inhibitor

摘要

An efficient synthesis of the potent KDR inhibitor 3-[5-[[4-(methylsulfonyl)-1-piperazinyl]methyl]-1H-indole-2-yl]quinolin-2(1H)-one(1)is described.The process features a noncryogenic indole boronation and a dicyclohexylamine-mediated Suzuki coupling.