HuagongsheHuagongshe Chemie-Druckbericht · Nur für Forschungszwecke
Water → 4-(4-Acetoxy-4-(4-chlorophenyl)-1-piperidinyl)-1-(4-fluorophenyl)-1-butanone
Beteiligte Stoffe
| Rolle | Name | HCID | Einwaage |
|---|---|---|---|
| Edukt | Water | HCID 962 | — |
| Edukt | Haloperidol | HCID 3559 | — |
| Edukt | Acetic Anhydride | HCID 7918 | — |
| Lösungsmittel | Pyridine | HCID 1049 | — |
| Produkt | 4-(4-Acetoxy-4-(4-chlorophenyl)-1-piperidinyl)-1-(4-fluorophenyl)-1-butanone | HCID 23364995 | — |
Reaktionsschritte
4-(4-(4-Chlorophenyl)-4-hydroxy-1-piperidinyl)-1-(4-fluorophenyl)-1-butanone (20 g) and acetic acid anhydride (16 g) in 200 ml of dried pyridine (KOH pellets) were refluxed for 2 h. The mixture was poured into cold H2O (0° C.) (2 liters) and extracted with isopropylether (2×200 ml). The combined organic phases were dried (MgSO4) and the solvent evaporated. The title compound was obtained after column chromatography on silica gel (eluent, ethyl acetate/dichloromethane/methanol, 1:1:1). Yield 10.6 g (48%). Mp 106°-110° C. (from isopropyl ether). The hydrochloride salt was precipitated from acetone. Mp 215° C. According to TLC analysis the content of Haloperidol was 0.5%.
Herkunft & Nachweise
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patentnummer | US04855307 |
| Quelldatensatz | uspto-grants-1989_08 |
| ORD ID | ord-53776443e02a432395057d3a40d75a82 |
| Quellennotiz | uspto-grants-1989_08 |