Design and chemical synthesis of [1, 2, 4] triazol [1, 5-c] pyrimidin-5-yl amines, a novel class of VEGFR-2 kinase inhibitors

…, NB Chernisheva, LK Salamandra, VV Semenov

文献索引：Kiselyov, Alexander S.; Piatnitski Chekler, Eugene L.; Chernisheva, Natalia B.; Salamandra, Lev K.; Semenov, Victor V. Tetrahedron Letters, 2009 , vol. 50, # 27 p. 3809 - 3812

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被引用次数: 6

摘要

The Letter describes a facile approach to 7, 8-dihydro [1, 2, 4] triazol [1, 5-c] pyrimidin-5-yl amines, a novel class of potent inhibitors of vascular endothelial growth factor receptor II (VEGFR-2). The synthetic sequence is centered around preparation of the key 3 (5)- cyanomethyl-1, 2, 4-triazole intermediates and their Knoevenagel condensation with aromatic aldehydes. A subsequent three-step conversion of Knoevenagel adducts ...