HuagongsheHuagongshe Chemie-Druckbericht · Nur für Forschungszwecke
Amlodipine → 4-(2-Chlorophenyl)-3-ethoxycarbonyl-5-methoxycarbonyl-6-methyl-2-[2-(3,4-dihydro-4-oxo-pyrimidin-2-ylamino)ethoxymethyl]-1,4-dihydropyridine
Beteiligte Stoffe
| Rolle | Name | HCID | Einwaage |
|---|---|---|---|
| Edukt | Amlodipine | HCID 2162 | — |
| Edukt | 2-(Methylthio)-1H-pyrimidin-4-one | HCID 79823 | — |
| Lösungsmittel | Ethanol | HCID 702 | — |
| Produkt | 4-(2-Chlorophenyl)-3-ethoxycarbonyl-5-methoxycarbonyl-6-methyl-2-[2-(3,4-dihydro-4-oxo-pyrimidin-2-ylamino)ethoxymethyl]-1,4-dihydropyridine | HCID 20199195 | — |
Reaktionsschritte
2-[2-Aminoethoxymethyl]-3-ethoxycarbonyl-4-(2-chlorophenyl)-5-methoxycarbonyl-6-methyl-1,4-dihydropyridine (0.75 g) and 2-methylthio-3H-pyrimid-4-one (0.5 g) were dissolved in ethanol (5 ml) and heated under reflux for 20 hours. The solvent was evaporated and the residue was partitioned between ethyl acetate and water. The organic layer was separated, washed with 2N hydrochloric acid to remove any unreacted amine, and then with dilute sodium hydroxide solution. It was then washed with water, dried, filtered and evaporated to give a yellow gum. Chromatography on silica "Kieselgel 60H" (Trade Mark) eluting with ethyl acetate gave the title compound, which was recrystallised from ethyl acetate, yield 171 mg, m.p. 148°-150°.
Herkunft & Nachweise
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patentnummer | US04670449 |
| Quelldatensatz | uspto-grants-1987_06 |
| ORD ID | ord-d4d6a2ff3ba24990acb2c1263eeba5fd |
| Quellennotiz | uspto-grants-1987_06 |