Common name: Regorafenib; BAY 73-4506; Fluoro-Sorafenib; DAST; Regorafenib hydrate; Stivarga
Trademarks: Stivarga
Molecular Formula: C21H17ClF4N4O4
CAS Registry Number: 755037-03-7
CAS Name: 4-[4-({[4-Chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)-3-fluorophenoxy]-N-methylpyridine-2-carboxamide
Molecular Weight: 482.82
SMILES:CNC(=O)C1=CC(OC2=CC(F)=C(NC(=O)NC3=CC=C(Cl)C(=C3)C(F)(F)F)C=C2)=CC=N1
InChI Key: FNHKPVJBJVTLMP-UHFFFAOYSA-N
InChI:InChI=1S/C21H15ClF4N4O3/c1-27-19(31)18-10-13(6-7-28-18)33-12-3-5-17(16(23)9-12)30-20(32)29-11-2-4-15(22)14(8-11)21(24,25)26/h2-10H,1H3,(H,27,31)(H2,29,30,32)
Activity: Tyrosine Kinase Inhibitor; Protein Kinase Inhibitor; VEGFR-2 Kinase Inhibitor; KDR Kinase Inhibitor; TIE-2 Kinase Inhibitor; Metastatic Colorectal Cancer Therapy; Advanced Gastrointestinal Stromal Tumours Therapy; Dual Receptor Tyrosine Kinase Inhibitor; Oncolytic Drugs
Status: Launched 2012
Originator: Bayer
Regorafenib synthesis: WO2005009961A2
Regorafenib synthesis: WO2011128261A1
Regorafenib synthesis: Fine Chemical Intermediates, 2012, 6, 31-34
References:
1. Dumas, J.; et. al. Fluoro substituted omega-carboxyaryl diphenyl urea for the treatment and prevention of diseases and conditions. WO2005009961A2
2. Liu, Y.-F.; et. al. The Synthesis of Regorafenib. Fine Chemical Intermediates, 2012, 6, 31-34.
3. Stiehl, J.; et. al. Process for the preparation of 4- {4-[({[4-chloro-3-(trifluoromethyl)-phenyl]amino}carbonyl)amino]-3-fluorophenoxy}-n-methylpyridine-2-carboxamide, its salts and monohydrate. WO2011128261A1
