Beteiligte Stoffe
| Rolle | Name | HCID | Einwaage |
|---|
| Edukt | Water | HCID 962 | — |
| Edukt | Potassium Carbonate | HCID 11430 | — |
| Edukt | 4-(chloromethyl)-2-[(E)-2-[4-(trifluoromethyl)phenyl]ethenyl]-1,3-oxazole | HCID 9857126 | — |
| Edukt | 4-(4-[1,2,3]Triazol-1-yl-butyl)phenol | HCID 12109494 | — |
| Lösungsmittel | Methanol | HCID 887 | — |
| Lösungsmittel | Dimethylformamide | HCID 6228 | — |
| Produkt | Mubritinib | HCID 6444692 | 93% |
Reaktionsschritte
4-[4-(1H-1,2,3-Triazol-1-yl)butyl]phenol (400 mg, 1.84 mmol) and 4-(chloromethyl)-2-[(E)-2-[4-(trifluoromethyl)phenyl]ethenyl]-1,3-oxazole (529 mg, 1.84 mmol) were dissolved in dimethylformamide (3 ml) and potassium carbonate (279 mg, 2.02 mmol) was added. The mixture was stirred at 65-75° C. for 4 hours. 4-[4-(1H-1,2,3-Triazol-1-yl)butyl]phenol (40 mg, 0.184 mmol) was added and the mixture was stirred at 65-75° C. for further 3 hours. The mixture was cooled to room temperature and water (5 ml) was added, then methanol (3 ml) was added. The mixture was stirred at room temperature for 40 min, and the precipitated crystals were collected by filtration and washed with water. The crystals were dried under reduced pressure to give 1-[4-[4-[[2-[(E)-2-[4-(trifluoromethyl)phenyl]ethenyl]-1,3-oxazol-4-yl]methoxy]phenyl]butyl]-1H-1,2,3-triazole (799 mg, yield 93%).
Herkunft & Nachweise
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| Patentnummer | US06743924B2 |
|---|
| Quelldatensatz | uspto-grants-2004_06 |
|---|
| ORD ID | ord-48ba846d4d674c9ab2d6e54c1c312e97 |
|---|
| Quellennotiz | uspto-grants-2004_06 |
|---|