Wednesday, December 3, 2014


Common name: Erlotinib; CP-358774; OSI-774, Erlotinib hydrochloride; Tarceva
Trademarks:  Tarceva (OSI)
Molecular Formula: C22H23N3O4
CAS Registry Number: 183321-74-6; 183319-69-9 (mono HCl)
CAS Name: N-(3-Ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine
Molecular Weight: 393.436
Activity:  Antineoplastic; Tyrosine Kinase Inhibitors, Protein Kinase Inhibitors

Erlotinib synthesis: US5747498

Erlotinib synthesis: US6476040

Erlotinib synthesis: Org Process Res Dev 2007, 11, 813-816

1. Schnur, R. C.; et. al. Treatment of hyperproliferative diseases. US5747498A
2. Norris, T.; et. al. Processes and intermediates for preparing anti-cancer compounds. US6476040B1.
3. Baumann, M.; et. al. An overview of the synthetic routes to the best selling drugs containing 6-membered heterocycles. Beilstein J Org Chem 2013, 9, 2265–2319.
4. Chandregowda, V.; et. al. Convergent Approach for Commercial Synthesis of Gefitinib and Erlotinib. Org Process Res Dev 2007, 11, 813–816.