Preparation of N-{3-chloro-4-[(3-fluorobenzyl)oxy]phenyl}-6-iodoquinazolin-4-amine_Kain Industrial Additive
[Overview] N-{3-Chloro-4-[(3-fluorobenzyl)oxy]phenyl}-6-iodoquinazolin-4-amine is an important intermediate in the synthesis of lapatinib. [Preparation method] 1. Use 2-aminobenzonitrile as raw material, iodide to obtain 2-amino-5-iodobenzonitrile, and then condense it with N,N-dimethylformamide dimethyl acetal (DMF?DMA) N’-(2-cyano-4-iodophenyl)-N,N-dimethylformamidine. Excess DMF?DMA was evaporated under reduced pressure, and glacial acetic acid and 3-chloro-4-[(3-fluorobenzyl)oxy]aniline were added to perform Dimroth rearrangement to obtain N-{3-chloro-4-[(3-…