HuagongsheHuagongshe Chemie-Druckbericht · Nur für Forschungszwecke
Potassium Carbonate → (R)-2-(4-cyano-3-(3-methylisothiazol-5-ylamino)phenylamino)-2-phenylacetamide
Beteiligte Stoffe
| Rolle | Name | HCID | Einwaage |
|---|---|---|---|
| Edukt | Potassium Carbonate | HCID 11430 | — |
| Edukt | Binap, (A+-)- | HCID 634876 | — |
| Edukt | 3-Methylisothiazol-5-ylamine hydrochloride | HCID 2723918 | — |
| Edukt | (R)-2-(3-bromo-4-cyanophenylamino)-2-phenylacetamide | HCID 67508351 | — |
| Katalysator | palladium(II) acetate | HCID 167845 | — |
| Lösungsmittel | 1,4-Dioxane | HCID 31275 | — |
| Produkt | (R)-2-(4-cyano-3-(3-methylisothiazol-5-ylamino)phenylamino)-2-phenylacetamide | HCID 67508197 | — |
Reaktionsschritte
A mixture of (R)-2-(3-bromo-4-cyanophenylamino)-2-phenylacetamide (78 mg, 0.236 mmol), 5-amino-3-methylisothiazole hydrochloride (47 mg, 0.312 mmol), BINAP (30 mg, 0.048 mmol), Pd(OAc)2 (20 mg, 0.089 mmol) and K2CO3 (134 mg, 0.971 mmol) in dioxane (3 mL) was degassed with Ar, then was stirred at 120 C for 18 h. Water and EtOAc were added. After being filtered, the organic phase was separated, washed with brine, dried over Na2SO4, concentrated in vacuo to give (R)-2-(4-cyano-3-(3-methylisothiazol-5-ylamino)phenylamino)-2-phenylacetamide as a crude residue.
Herkunft & Nachweise
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patentnummer | US08846928B2 |
| Quelldatensatz | uspto-grants-2014_09 |
| ORD ID | ord-1f34d6afa9a0402880ac381533fe2133 |
| Quellennotiz | uspto-grants-2014_09 |