One method of synthesis of the EGFR inhibitor Dacomitinib
2013
The present invention discloses a method for synthesizing Dacomitinib EGFR inhibitor, which is a 10-step synthesis method, firstly 2-amino-4-fluorobenzoic acid and formamide ring closure reaction at an elevated temperature, and then sequentially nitration, hydrogenated reduction, amidation reaction of the methoxy group chlorination reaction and, finally preparation of 3-chloro-4-fluoroaniline to give docking EGFR inhibitor Dacomitinib, according to the main starting material is easily available on the market are all close high molecular and high economic efficiency, green technology is an efficient method for industrial production.
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