Patent ID: 8853396

Claim:
A method for the preparation of Lapatinib of formula (I) or a salt thereof: comprising the steps of: (a) reacting of 6-iodoquinazolin-4-ol of formula (II): with 3,4-dihydro-2H-pyran to provide 6-iodo-4-(tetrahydro-2H-pyran-2-yloxy)quinazoline of formula (III): (b) reacting of 6-iodo-4-(tetrahydro-2H-pyran-2-yloxy)quinazoline of formula (III) with 2-formylfuran-5-boronic acid to provide 5-[4-(tetrahydro-2H-pyran-2-yloxy)quinazolin-6-yl]furan-2-carbaldehyde of formula (IV): (c) reacting of the intermediate of formula (IV) with 2-(methylsulfonyl)ethanamine to provide 2-(methylsulfonyl)-N-({5-[4-(tetrahydro-2H-pyran-2-yloxy)quinazolin-6-yl]furan-2-yl}methyl)ethanamine of formula (V): (d) deprotecting of the intermediate of formula (V) to provide 6-[5-({[2-(methylsulfonyl)ethyl]amino}methyl)furan-2-yl] quinazolin-4-ol of formula (VI): (e) converting of the intermediate of formula (VI) to provide N-{[5-(4-substituted-quinazolin-6-yl)furan-2-yl]methyl}-2-(methylsulfonyl) ethanamine of formula (VII): in which X is selected from the group consisting of: fluorine, chlorine, bromine, iodine, O-Ms (mesilate), and O-Ts (tosilate), O-Tf (triflate); (f) reacting of the intermediate of formula (VII) with 3-chloro-4-[(3-fluorobenzyl)oxy]aniline of formula (VIII): to provide Lapatinib of formula (I):