Author/Authors :
Erickson، نويسنده , , Greg and Guo، نويسنده , , Jiasheng and McClure، نويسنده , , Mike and Mitchell، نويسنده , , Mark and Salaun، نويسنده , , Marie-Catherine and Whitehead، نويسنده , , Andrew، نويسنده ,
Abstract :
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.
Keywords :
C–H activation , Lapatinib , Pivalic acid , Direct arylation , palladium acetate
