Quinazolines Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor Synthesis Research

The development of a receptor-tyrosine kinase inhibitor(RTKs) and epidermal growth factor receptor (EGFR) were reviewed. And epidermal growth factor receptor(EGFR) tyrosine kinase inhibitors were introduced in detail. Iressa is the first EGFR as a tyrosine kinase inhibitor. We initially designed the modifications of 4, 6 and 7 positions of quinazoline nucleu with Iressa as the lead compound, under preserving the quinazoline nucleu, based on the analysis of structure-activity relationship (SAR) of quinazoline derivatives. As a result, twenty-five new compounds were synthesized from 3-hydroxy-4-methoxybenzoic acid and 3-methoxy-4-hydroxybenzoic acid. The structures of the target compounds were confirmed by MS, ~1H-NMR and IR (CL-1, CL-14, CL-16)...