Saturday, January 17, 2015


Common name: Bosutinib; SKI-606; Bosulif; Bosutinib hydrate
Trademarks:  Bosulif
Molecular Formula: C26H29Cl2N5O3 
CAS Registry Number: 380843-75-4
CAS Name: 4-[(2,4-dichloro-5-methoxyphenyl)amino]-6-methoxy-7-[3-(4-methylpiperazin-1-yl)propoxy]quinoline-3-carbonitrile
Molecular Weight: 530.446
Activity: Tyrosine Kinase Inhibitor; Protein Kinase Inhibitor;  Bcr-Abl Kinase Inhibitor; SRC family Kinases Inhibitor; Chronic Myelogenous Leukemia Therapy; CML Therapy; Dual Inhibitor of Src and Abl Kinases

Bosutinib synthesis: US20050043537A1 (new version with the same raw material in Ref. 3)

Bosutinib synthesis: J Med Chem 200144(23), 3965-3977

Bosutinib synthesis: Molecules 2010, 15, 4261-4266

1. Sutherland, K.; Boschelli D. H.; et. al. Amidation of cyanoacetic acid with an acid catalyst, condensation of the cyanoacetamide with aniline, an alcohol solvent, and a trialkylorthoformate, cyclization of the 3-amino-2-cyanoacrylamide; mild conditions; protein kinase inhibitors. US20050043537A1
2. Li, F.; et. al. Synthesis of Bosutinib from 3-Methoxy-4-hydroxybenzoic Acid. Molecules 2010, 15, 4261-4266.
3. Vaidyanathan, R.; et. al. A Robust, Streamlined Approach to Bosutinib Monohydrate. Org Process Res Dev 2013, 17, 500-504.
4. Boschelli D. H.; et. al. Optimization of 4-phenylamino-3-quinolinecarbonitriles as potent inhibitors of Src kinase activity. J Med Chem 2001, 44(23), 3965-3977.
5. Boschelli D. H.; et. al. 4-[(2,4-dichloro-5-methoxyphenyl)amino]-6-alkoxy-3-quinolinecarbonitriles for the treatment of ischemic injury. WO2004075898A1
6. Boschelli D. H.; et. al. 7-Alkoxy-4-phenylamino-3-quinolinecar-bonitriles as dual inhibitors of Src and Abl kinases. J Med Chem 2004, 47(7), 1599-601.