845271-73-0Relevant articles and documents
Synthesis of Lapatinib via direct regioselective arylation of furfural
Erickson, Greg,Guo, Jiasheng,McClure, Mike,Mitchell, Mark,Salaun, Marie-Catherine,Whitehead, Andrew
, p. 6007 - 6010 (2014)
A new synthesis of Lapatinib, an orally active drug for breast cancer, is described. The synthesis involves a palladium catalyzed regioselective arylation of furfural with 6-bromo-N-(3-chloro-4-((3-fluorobenzyl)oxy)phenyl)quinazolin-4-amine. This key step replaces an atom inefficient Suzuki cross coupling reaction used in a previously disclosed route and significantly shortens the synthesis.