Beteiligte Stoffe
| Rolle | Name | HCID | Einwaage |
|---|
| Edukt | Hydrochloric Acid | HCID 313 | — |
| Edukt | 4-Amino-3,5-dichloropyridine | HCID 89888 | — |
| Edukt | Potassium | HCID 5462222 | — |
| Edukt | 3-(Cyclopropylmethoxy)-4-(difluoromethoxy)benzoyl chloride | HCID 12047330 | — |
| Lösungsmittel | Water | HCID 962 | — |
| Lösungsmittel | Dimethylformamide | HCID 6228 | — |
| Produkt | Roflumilast | HCID 449193 | — |
Reaktionsschritte
The potassium salt suspension of the anion of 4-amino-3,5-dichloropyridine in DMF (2-2.5 equivalents) is introduced into a reaction vessel. A solution of 3-cyclopropylmethoxy-4-difluoromethoxybenzoyl chloride (1 equivalent) in DMF is slowly added to this suspension while stirring vigorously at a temperature of 15 to 40° C., preferably 20 to 30° C. After the reaction is complete, water is slowly added while stirring at 15-25° C., and the pH is adjusted to 2-3 with hydrochloric acid.
Herkunft & Nachweise
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| Patentnummer | US07470791B2 |
|---|
| Quelldatensatz | uspto-grants-2008_12 |
|---|
| ORD ID | ord-93dc10d56d904d7695b2396e89a05a81 |
|---|
| Quellennotiz | uspto-grants-2008_12 |
|---|
