Two benzoxazinone compounds as epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors were synthesized and characterized by NMR and high-resolution mass spectrometry (HRMS). An efficient chlorination method was introduced in the synthesis of 4-chloro-2-oxo-2H -benzoxazinone-6-yl acetate. The inhibition activities of the target compounds and the important intermediates for EGFR tyrosine kinase activity in vitro were determined.
