HuagongsheHuagongshe Chemie-Druckbericht · Nur für Forschungszwecke
5-Amino-3-methylisoxazole → (R)-2-(4-cyano-3-(3-methylisoxazol-5-ylamino)phenylamino)-4-methylpentanamide
Beteiligte Stoffe
| Rolle | Name | HCID | Einwaage |
|---|---|---|---|
| Edukt | 5-Amino-3-methylisoxazole | HCID 84590 | — |
| Edukt | 1,1'-(9,9-Dimethyl-9H-xanthene-4,5-diyl)bis(1,1-diphenylphosphine) | HCID 636044 | — |
| Edukt | Sodium Phenoxide Trihydrate | HCID 23681143 | — |
| Edukt | (R)-2-(3-bromo-4-cyanophenylamino)-4-methylpentanamide | HCID 67509372 | — |
| Katalysator | Bis(dibenzylideneacetone)palladium | HCID 9811564 | — |
| Lösungsmittel | 1,4-Dioxane | HCID 31275 | — |
| Produkt | (R)-2-(4-cyano-3-(3-methylisoxazol-5-ylamino)phenylamino)-4-methylpentanamide | HCID 67508850 | 15,8% |
Reaktionsschritte
A mixture of (R)-2-(3-bromo-4-cyanophenylamino)-4-methylpentanamide (120 mg, 0.387 mmol), 5-amino-3-methylisoxazole (60 mg, 0.612 mmol), sodium phenoxide trihydrate (100 mg, 0.588 mmol), xantphos (25 mg, 0.043 mmol) and Pd2(dba)3 (20 mg, 0.021 mmol) in dioxane (3 mL) was degassed with Ar, then was heated at 170 C for 15 min by microwave. It was concentrated in vacuo. The residue was purified by HPLC to give (R)-2-(4-cyano-3-(3-methylisoxazol-5-ylamino)phenylamino)-4-methylpentanamide (20 mg).
Herkunft & Nachweise
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patentnummer | US09359375B2 |
| Quelldatensatz | uspto-grants-2016_06 |
| ORD ID | ord-43dbeeb0433343a2ba9a7895bc10168b |
| Quellennotiz | uspto-grants-2016_06 |