Synthesis Of Quinazoline Tyrosine Kinase Receptor Inhibitors

The development of a receptor-tyro sine kinase inhibitor ( RTKs ) and epidermal growth factor receptor (EGFR) were reviewed. And epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors were introduced in detail.Gefitinib is the first EGFR as a tyrosine kinase inhibitor. We initially designed the modifications of 4 and 7 positions of quinazoline nucleu with Gefitinib 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 new compounds were synthesized from 2-amino-4-nitrobenzoic acid. The structures of the target compounds were confirmed by MS, ~1H-NMR .