Beteiligte Stoffe
| Rolle | Name | HCID | Einwaage |
|---|
| Edukt | Pyrazole | HCID 1048 | — |
| Edukt | Cesium carbonate | HCID 10796 | — |
| Edukt | 5-Amino-2-fluoropyridine | HCID 819440 | — |
| Lösungsmittel | Chloroform | HCID 6212 | — |
| Lösungsmittel | N-methyl-2-pyrrolidone | HCID 13387 | — |
| Produkt | 6-(1H-pyrazol-1-yl)pyridin-3-amine | HCID 16774822 | 17% |
Reaktionsschritte
Commercial 6-fluoropyridin-3-amine (500 mg, 4.46 mmol) was dissolved in 20 mL dry NMP. To it were added pyrazole (910 mg, 13.4 mmol) and cesium carbonate (4.4 g, 13.4 mmol). The mixture was stirred in a sealed tube at 120° C. for over the weekend (3 nights). The mixture was diluted with chloroform, washed with brine (3 times), dried, concentrated and subjected to flash column (0 to 30% EtOAc in DCM) to isolate 6-(1H-pyrazol-1-yl)pyridin-3-amine (120 mg, 17% yield).
Herkunft & Nachweise
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| Patentnummer | US08846928B2 |
|---|
| Quelldatensatz | uspto-grants-2014_09 |
|---|
| ORD ID | ord-b211c993c0db4887b1819cb46fe63efb |
|---|
| Quellennotiz | uspto-grants-2014_09 |
|---|