320337-19-7

Upstream product

• 5847-59-6 2-bromo-4-nitrophenol 
• 320337-15-3 4-benzyloxy-3-bromoaniline 
• 98556-31-1 4-chloro-6-iodoquinazoline 
• 100-39-0 benzyl bromide 
• 191602-86-5 1-(benzyloxy)-2-bromo-4-nitrobenzene 

Downstream Products

• 320337-28-8 5-(4-(3-Bromo-4-(benzyloxy)-anilino)-quinazolin-6-yl)-furan-2-carbaldehyde 

Relevant academic research and scientific papers

Optimization and SAR for dual ErbB-1/ErbB-2 tyrosine kinase inhibition in the 6-furanylquinazoline series

Synthetic modifications on a 6-furanylquinazoline scaffold to optimize the dual ErbB-1/ErbB-2 tyrosine kinase inhibition afforded consistent SAR whereby a 4-(3-fluorobenzyloxy)-3-haloanilino provided the best enzyme potency and cellular selectivity. Changes made to the 6-furanyl group had little impact on the enzyme activity, but appeared to dramatically affect the cellular efficacy. The discovery of lapatinib emerged from this work.

Anilinoquinazolines as protein tyrosine kinase inhibitors

Heteroaromatic compounds are described, methods for their preparation, pharmaceutical compositions containing them, methods of use, and their use in medicines. In particular, the invention relates to quinazoline and pyridopyrimidine derivatives which exhibit protein tyrosine kinase inhibition.