HuagongsheHuagongshe Chemie-Druckbericht · Nur für Forschungszwecke
Water → (R)-2-(5-bromo-4-cyano-2-fluorophenylamino)-4-methylpentanamide
Beteiligte Stoffe
| Rolle | Name | HCID | Einwaage |
|---|---|---|---|
| Edukt | Water | HCID 962 | — |
| Edukt | Diisopropylethylamine | HCID 81531 | — |
| Edukt | 2-Bromo-4,5-difluorobenzonitrile | HCID 19261277 | — |
| Edukt | (R)-2-Amino-4-methylpentanamide hydrochloride | HCID 56776963 | — |
| Lösungsmittel | Dimethyl Sulfoxide | HCID 679 | — |
| Lösungsmittel | Ethyl Acetate | HCID 8857 | — |
| Produkt | (R)-2-(5-bromo-4-cyano-2-fluorophenylamino)-4-methylpentanamide | HCID 67508329 | 53,3% |
Reaktionsschritte
A solution of 2-bromo-4,5-difluorobenzonitrile (218 mg, 1.00 mmol), D-leucine amide hydrochloride (185 mg, 1.10 mmol) and DIEA (0.600 mL, 3.45 mmol) in DMSO (3 mL) was stirred at 120 C for 18 h. Water and EtOAc were added. The organic phase was separated, washed with water, dried over Na2SO4, concentrated in vacuo. The residue was purified by a silica gel column, eluted with 0-50% EtOAc in hexane to give (R)-2-(5-bromo-4-cyano-2-fluorophenylamino)-4-methylpentanamide (175 mg).
Herkunft & Nachweise
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patentnummer | US09359375B2 |
| Quelldatensatz | uspto-grants-2016_06 |
| ORD ID | ord-56997fa30bd34480b2ab386834b9a509 |
| Quellennotiz | uspto-grants-2016_06 |