HuagongsheHuagongshe Chemie-Druckbericht · Nur für Forschungszwecke
Potassium Carbonate → (R)-2-(5-cyano-6-(4-(pyridin-3-yl)phenylamino)pyrazin-2-ylamino)butanamide
Beteiligte Stoffe
| Rolle | Name | HCID | Einwaage |
|---|---|---|---|
| Edukt | Potassium Carbonate | HCID 11430 | — |
| Edukt | 4-(Pyridin-3-yl)aniline | HCID 459522 | — |
| Edukt | Binap, (A+-)- | HCID 634876 | — |
| Edukt | (R)-2-(6-chloro-5-cyanopyrazin-2-ylamino)butanamide | HCID 86685581 | — |
| Katalysator | palladium(II) acetate | HCID 167845 | — |
| Lösungsmittel | 1,4-Dioxane | HCID 31275 | — |
| Produkt | (R)-2-(5-cyano-6-(4-(pyridin-3-yl)phenylamino)pyrazin-2-ylamino)butanamide | HCID 86685585 | 57,8% |
Reaktionsschritte
A mixture of (R)-2-(6-chloro-5-cyanopyrazin-2-ylamino)butanamide (100 mg, 0.417 mmol), 4-(pyridin-3-yl)aniline (77 mg, 0.452 mmol), K2CO3 (100 mg, 0.724 mmol), BINAP (30 mg, 0.048 mmol) and Pd(OAc)2 (15 mg, 0.066 mmol) in dioxane (3 mL) was degassed with Ar, then was stirred at 110 C for 20 h. The mixture was concentrated in vacuo. The residue was purified by HPLC to give (R)-2-(5-cyano-6-(4-(pyridin-3-yl)phenylamino)pyrazin-2-ylamino)butanamide (90 mg).
Herkunft & Nachweise
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patentnummer | US08877760B2 |
| Quelldatensatz | uspto-grants-2014_11 |
| ORD ID | ord-7f8633bf2a204d9abc95189d4f933d76 |
| Quellennotiz | uspto-grants-2014_11 |