p-Toluenesulfonic acid → Sorafenib Tosylate

HRID 1913897

Reaktionsgleichung

Reaktionsgleichung von HRID 1913897
[CH3:1][NH:2][C:3]([C:5]1[CH:6]=[C:7]([O:11][C:12]2[CH:13]=[CH:14][C:15]([NH:18][C:19]([NH:21][C:22]3[CH:23]=[CH:24][C:25]([Cl:32])=[C:26]([C:28]([F:31])([F:30])[F:29])[CH:27]=3)=[O:20])=[CH:16][CH:17]=2)[CH:8]=[CH:9][N:10]=1)=[O:4].[C:33]1([CH3:43])[CH:38]=[CH:37][C:36]([S:39]([OH:42])(=[O:41])=[O:40])=[CH:35][CH:34]=1>O>[CH3:43][C:33]1[CH:38]=[CH:37][C:36]([S:39]([OH:42])(=[O:41])=[O:40])=[CH:35][CH:34]=1.[CH3:1][NH:2][C:3]([C:5]1[CH:6]=[C:7]([O:11][C:12]2[CH:17]=[CH:16][C:15]([NH:18][C:19]([NH:21][C:22]3[CH:23]=[CH:24][C:25]([Cl:32])=[C:26]([C:28]([F:31])([F:29])[F:30])[CH:27]=3)=[O:20])=[CH:14][CH:13]=2)[CH:8]=[CH:9][N:10]=1)=[O:4]

Komponenten

4

Edukt 2

HCID 6101p-Toluenesulfonic acidHCID 216239Sorafenib

Produkt 1

HCID 406563Sorafenib TosylateAusbeute 85,5 %

Reagenzien, Katalysatoren, Lösungsmittel 1

HCID 962WaterLösungsmittel

Reaktionsbedingungen

Temperatur
30 °C

Versuchsvorschrift

Sorafenib free base (3 g) was added to a solution of p-toluenesulphonic acid (14.4 g) in water (6 mL). The reaction mixture was stirred at about 30° C. for about 2 hours. The reaction mixture was filtered, washed with water (2×10 mL) and dried under reduced pressure at about 70° C. for about 12 hours to obtain sorafenib tosylate.

Aufarbeitung

  1. filtrationThe reaction mixture was filtered
  2. washwashed with water (2×10 mL)
  3. customdried under reduced pressure at about 70° C. for about 12 hours

Quellen und Nachweise

ORD-Eintrag
ord-0e59618d4303487fbd46294dddc01eab
Quelldatensatz
uspto-grants-2013_12
Patentnummer
US08609854B2

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