期刊
TETRAHEDRON
卷 62, 期 6, 页码 1110-1115出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tet.2005.10.081
关键词
KDR; Pd-catalysis; Xantphos; aminothiazole; chloropyridine; piperazine
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.
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