AN IMPROVED PROCESS FOR THE PREPARATION OF GEFITINIB

摘要

The present invention relates to a modified process for preparing Gefitinib (4-(3′-chloro-4′-fluoroanilino)-7-methoxy-6-(3-morpholinopropoxy)quinazoline) represented by chemical formula I, which provides high cost-efficiency, high yield and high purity. More particularly, the present invention provides a modified process for preparing Gefitinib, which comprises carrying out condensation of 4-(3′-chloro-4-fluoroanilino)-7-methoxyquinazolin-6-ol represented by chemical formula II with 3-morpholinopropyl chloride represented by chemical formula III in the presence of an inorganic basic compound by using an alkali metal iodide and 18-crown-6 as a catalyst.