HuagongsheHuagongshe Chemie-Druckbericht · Nur für Forschungszwecke
Cyclohexene → N-[5-(3,5-difluorobenzyl)-1H-indazol-3-yl]-4-amino-2-[tetrahydro-2H-pyran-4-yl(trifluoroacetyl)amino]benzamide
Beteiligte Stoffe
| Rolle | Name | HCID | Einwaage |
|---|---|---|---|
| Edukt | Cyclohexene | HCID 8079 | — |
| Edukt | N-[5-(3,5-difluorobenzyl)-1H-indazol-3-yl]-4-nitro-2-[tetrahydro-2H-pyran-4-yl(trifluoroacetyl)amino]benzamide | HCID 86647627 | — |
| Katalysator | Palladium | HCID 23938 | — |
| Lösungsmittel | 1,4-Dioxane | HCID 31275 | — |
| Produkt | N-[5-(3,5-difluorobenzyl)-1H-indazol-3-yl]-4-amino-2-[tetrahydro-2H-pyran-4-yl(trifluoroacetyl)amino]benzamide | HCID 86647628 | 82% |
Reaktionsbedingungen
| Temperatur | 100 °C |
|---|
Reaktionsschritte
A mixture of N-[5-(3,5-difluorobenzyl)-1H-indazol-3-yl]-4-nitro-2-[tetrahydro-2H-pyran-4-yl(trifluoroacetyl)amino]benzamide (3.86 g, 6.4 mmol), cyclohexene (10 mL), dioxane (70 mL) and 10% Pd/C (0.42 g) was stirred at 100° C. for 4 hours. The reaction mixture was filtered over a celite pad washing thoroughly with THF and MeOH. After evaporation of the organic phase, purification of the crude by chromatography over silica gel (DCM/EtOH 9/1) gave 2.75 g of title compound (82% yield).
Herkunft & Nachweise
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patentnummer | US09102662B2 |
| Quelldatensatz | uspto-grants-2015_08 |
| ORD ID | ord-81c2bf587aea4e6e84516bdab721ca45 |
| Quellennotiz | uspto-grants-2015_08 |