This paper deals with the development of a practical process for lapatinib tosylate monohydrate(〖STHZ〗1〖STBZ〗)，a molecule-targeted antitumor agent.The target product 1 was synthesized from commercially available 6-iodoquinazolin-4-one(3 in a five-step process with an overall yield of 48% via chlorination(88% yield)，palladium carbon catalyzed Suzuki coupling with 5-formyl-2-furylboronic acid(96% yield)，reductive amination with 2-(methylsulfone)ethylamine(94% yield)，salt formation with p-toluenesulfonic acid monohydrate(87% yield)，and final crystallization from THF-water (8∶2) (70% yield).The intermediates and the target product were characterized by melting points，¹H NMR，¹³C NMR，and ESI-MS.During our optimized process，chromatography，large excess of chlorinating agent and halogenated solvent that are unfriendly to the environment were all removed；expensive and difficult-to-handle homogeneous catalyst was successfully substituted with heterogeneous catalyst palladium carbon which could be recovered easily.In conclusion，this streamlined synthetic process of lapatinib tosylate monohydrate(1) highlights excellent yield in almost every procedure，ease of operation，robustness，as well as green chemistry，and thus should be amenable to large-scale production.