Tetrahedron letters

Facile synthesis of 7-amino anilinoquinazolines via direct amination of the quinazoline core

CS Harris, JG Kettle, EJ Williams

Index: Harris, Craig S.; Kettle, Jason G.; Williams, Emma J. Tetrahedron Letters, 2005 , vol. 46, # 43 p. 7381 - 7384

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Citation Number: 20

Abstract

In our recent efforts to explore variation at positions 6 and 7 of the ring nucleus to further investigate the structure–activity, it was shown that 4-(3-chloro-4-fluoroanilino)-6-alkoxy-7-aminoquinazolines were inhibitors of the tyrosine kinase activity of EGFR. Herein, we communicate the facile and parallel chemistry employed to achieve this important class of kinase inhibitors from their corresponding 7-triflates (Scheme 1). ... Synthesis of the 7-triflates 3 and 5. Reagents and conditions: (i) ...