Synthetic Communications

Synthesis of novel benzoxazinone compounds as epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors

S Chen, X Li, S Wan, T Jiang

Index: Chen, Shaopeng; Li, Xuemin; Wan, Shengbiao; Jiang, Tao Synthetic Communications, 2012 , vol. 42, # 19 p. 2937 - 2946

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Citation Number: 9

Abstract

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.