A very concise synthesis of a potent N-(1,3-thiazol-2-yl)pyridin-2-amine KDR kinase inhibitor

A very concise synthesis of a potent KDR kinase inhibitor 1 is described. The synthesis features an exceedingly efficient one-potpreparation of the aminothiazole 6 followed by Pd-Xantphos catalyzed cross-coupling with chloropyridine aldehyde 11. Reductive amination of the resulting aldehyde 10 with the piperazine fragment 9 afforded the final product. (c) 2005 Elsevier Ltd. All rights reserved.