Regorafenib monohydrate

Regorafenib monohydrate Struktur
1019206-88-2
CAS-Nr.
1019206-88-2
Englisch Name:
Regorafenib monohydrate
Synonyma:
Regorafenib H2O;Regorafenib hydrate;Regfenib monohydrate;Regorafenib (200 mg);Refined Sunflower Oil;BAY 73-4506 Monohydrate;Regorafenib monohydrate;Regorafenibhydrate USP/EP/BP;Regorafenib (BAY 73-4506)Monohydrate;Regorafenib monohydrate (BAY 73-4506)
CBNumber:
CB52641189
Summenformel:
C21H17ClF4N4O4
Molgewicht:
500.83
MOL-Datei:
1019206-88-2.mol

Regorafenib monohydrate Eigenschaften

storage temp. 
2-8°C
Löslichkeit
≥25.05 mg/mL in DMSO; insoluble in H2O
Aggregatzustand
solid
Sicherheit
  • Risiko- und Sicherheitserklärung
  • Gefahreninformationscode (GHS)
Bildanzeige (GHS) GHS hazard pictogramsGHS hazard pictograms
Alarmwort Warnung
Gefahrenhinweise
Code Gefahrenhinweise Gefahrenklasse Abteilung Alarmwort Symbol P-Code
H373 Kann die Organe schädigen bei längerer oder wiederholter Exposition. Spezifische Zielorgan-Toxizität (wiederholte Exposition) Kategorie 2 Warnung P260, P314, P501
H410 Sehr giftig für Wasserorganismen mit langfristiger Wirkung. Langfristig (chronisch) gewässergefährdend Kategorie 1 Warnung P273, P391, P501
Sicherheit
P201 Vor Gebrauch besondere Anweisungen einholen.
P273 Freisetzung in die Umwelt vermeiden.
P308+P313 BEI Exposition oder falls betroffen: Ärztlichen Rat einholen/ärztliche Hilfe hinzuziehen.

Regorafenib monohydrate Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung

Regorafenib monohydrate (BAY 73-4506) is an orally active and potent multi-targeted receptor tyrosine kinase inhibitor with potent anti-tumour and anti-angiogenic activity. It is approved for the treatment of metastatic colorectal cancer, advanced gastrointestinal mesenchymal stromal tumours and hepatocellular carcinoma.

Clinical Use

Regorafenib was approved by the U.S. Food and Drug Administration (FDA) in September 2012 for the treatment of metastatic colorectal cancer in patients who have previously undergone fluoropyrimidine-, oxaliplatin-, and irinotecan-based therapies. The FDA expanded the approved use of the drug to include patients with advanced gastrointestinal stromal tumors (GIST) that cannot be surgically removed and no longer respond to imatinib and sunitinib, two other drugs approved for treatment of GIST. Regorafenib, marketed under the trade name Stivarga®, was discovered and developed by Bayer Pharmaceuticals and marketed jointly with Onyx Pharmaceuticals. The active metabolites of the drug inhibit multiple targets within a variety of kinase families including those in the RET, VEGF, FGFR, PTK, and Abl pathways.

Synthese

Among several published synthesis, the most likely process scale synthesis will be highlighted from the two published syntheses, and this is described in the scheme. Commercially available picolinic acid (148) was heated with thionyl chloride to provide the crude intermediate 4-chloro-2- pyridyl acid chloride which was subsequently reacted with aqueous methyl amine in toluene to give 4- chloro-2-methylcarboxamide as its hydrochloride salt 149 in quantitative yield after treatment with acetyl chloride in toluene and ethanol. The hydrochloride salt was free based with sodium hydroxide and then immediately reacted with imine 150 (formed upon exposure to 4-amino-3-fluorophenol (153) in refluxing 3-methyl 2-butanone) in base to provide diaryl ether 151 in 84% yield. Reaction of amine 151 with the commercially available isocyanate 152 ultimately delivered regorafenib hydrate (XXIII) in 83% yield.

Synthesis_1019206-88-2

Regorafenib monohydrate Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte


Regorafenib monohydrate Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

Global( 238)Lieferanten
Firmenname Telefon E-Mail Land Produktkatalog Edge Rate
Yangzhou Qinyuan Pharmatech Co.,ltd
+86-18752526868
jennysun@yzqyyykj.com China 64 58
Hebei Yanxi Chemical Co., Ltd.
+8617531190177
peter@yan-xi.com China 5990 58
Capot Chemical Co.,Ltd.
571-85586718 +8613336195806
sales@capotchem.com China 29797 60
Beijing Cooperate Pharmaceutical Co.,Ltd
010-60279497
sales01@cooperate-pharm.com CHINA 1811 55
Henan Tianfu Chemical Co.,Ltd.
+86-0371-55170693 +86-19937530512
info@tianfuchem.com China 21700 55
Nanjing ChemLin Chemical Industry Co., Ltd.
025-83697070
product@chemlin.com.cn CHINA 3012 60
ATK CHEMICAL COMPANY LIMITED
+undefined-21-51877795
ivan@atkchemical.com China 32480 60
Anqing Chico Pharmaceutical Co., Ltd.
15380796838
chloewu@chicopharm.cn CHINA 341 58
career henan chemical co
+86-0371-86658258
sales@coreychem.com China 29914 58
Zhejiang ZETian Fine Chemicals Co. LTD
18957127338
stella@zetchem.com China 2141 58

1019206-88-2()Verwandte Suche:


  • 4-[4-[[[[4-Chloro-3-(trifluoromethyl)phenyl]amino]carbonyl]amino]-3-fluorophenoxy]-N-methyl-2-pyridinecarboxamide hydrate
  • Regorafenib monohydrate
  • Regorafenib (BAY 73-4506)Monohydrate
  • Regorafenib hydrate
  • BAY 73-4506 Monohydrate
  • Regorafenib monohydrate 4-[4-[[[[4-Chloro-3-(trifluoromethyl)phenyl]amino]carbonyl]amino]-3-fluorophenoxy]-N-methyl-2-pyridinecarboxamide hydrate
  • 4-[4-({[4-Chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)-3-fluorophenoxy]-N-methyl-2-pyridinecarboxamide hydrate (1:1)
  • 4-[4-[[4-chloro-3-(trifluoromethyl)phenyl]carbamoylamino]-3-fluorophenoxy]-N-methylpyridine-2-carboxamide,hydrate
  • Regorafenib monohydrate (BAY 73-4506)
  • Regorafenib H2O
  • 4-(4-(3-(4-chloro-3-(trifluoromethyl)phenyl)ureido)-3-fluorophenoxy)-N-methylpicolinamide hydrate
  • Regorafenibhydrate USP/EP/BP
  • 4-[4-[[[[4-Chloro-3-(trifluoromethyl)phenyl]amino]carbonyl]amino]-3-fluorophenoxy]-N-methyl-2-pyridinecarboxamide hydrate USP/EP/BP
  • 4-[4-[[[[4-Chloro-3-(trifluoromethyl)phenyl]amino]carbonyl]amino]-3-fluorophenoxy]-N-methyl-2-pyridi
  • Refined Sunflower Oil
  • Regfenib monohydrate
  • Regorafenib (200 mg)
  • 1019206-88-2
  • C21H15ClF4N4O3H2O
  • C21H17ClF4N4O4
  • API
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