HuagongsheHuagongshe Chemie-Druckbericht · Nur für Forschungszwecke
Iodoethane → 3-(2,3-Difluorophenyl)-1-ethylpyrrolidin-3-ol
Beteiligte Stoffe
| Rolle | Name | HCID | Einwaage |
|---|---|---|---|
| Edukt | Iodoethane | HCID 6340 | — |
| Edukt | Morpholine | HCID 8083 | — |
| Edukt | 1-Benzyl-3-(2,3-difluorophenyl)pyrrolidin-3-ol | HCID 68515849 | — |
| Lösungsmittel | Dimethylformamide | HCID 6228 | — |
| Produkt | 3-(2,3-Difluorophenyl)-1-ethylpyrrolidin-3-ol | HCID 25145776 | — |
Reaktionsschritte
Preparation according to Example 34: (+)-1-benzyl-3-(2,3-difluorophenyl)pyrrolidin-3-ol (0.40 g, 1.38 mmol), dimethyl formamide (3 mL), iodoethane (1.1 mL, 13.8 mmol) and morpholine (2 mL). Purification by HPLC on Waters OBD C18, 5 μm (MeOH/33 mM NH3, 20:80 to 45:55). Yield: 0.11 g. [α]D=+19.8° (methanol). The amine was converted to the fumaric acid salt and recrystallized from methanol/diethyl ether/diisopropyl ether: M.p. 118-120° C.; MS m/z (relative intensity, 70 eV) 228 (M+, 14), 141, (16), 127 (14), 72 (26), 71 (bp).
Herkunft & Nachweise
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patentnummer | US08188301B2 |
| Quelldatensatz | uspto-grants-2012_05 |
| ORD ID | ord-628501d4d3254dca9a156d5318b05bbf |
| Quellennotiz | uspto-grants-2012_05 |