HuagongsheHuagongshe Chemie-Druckbericht · Nur für Forschungszwecke
Amlodipine → 2-[2-(-(S)-4-Benzyloxycarbonylamino-4-methoxycarbonylbutanamido)ethoxymethyl]-4-(2-chlorophenyl)-3-ethoxycarbonyl-5-methoxycarbonyl-6-methyl-1,4-dihydropyridine
Beteiligte Stoffe
| Rolle | Name | HCID | Einwaage |
|---|---|---|---|
| Edukt | Amlodipine | HCID 2162 | — |
| Edukt | 1-Hydroxybenzotriazole | HCID 75771 | — |
| Edukt | 1,3-Propanediamine, N'-(ethylcarbonimidoyl)-N,N-dimethyl-, monohydrochloride | HCID 2723939 | — |
| Edukt | (4S)-4-{[(benzyloxy)carbonyl]amino}-5-methoxy-5-oxopentanoic acid | HCID 2733408 | — |
| Lösungsmittel | Dichloromethane | HCID 6344 | — |
| Lösungsmittel | Triethylamine | HCID 8471 | — |
| Produkt | 2-[2-(-(S)-4-Benzyloxycarbonylamino-4-methoxycarbonylbutanamido)ethoxymethyl]-4-(2-chlorophenyl)-3-ethoxycarbonyl-5-methoxycarbonyl-6-methyl-1,4-dihydropyridine | HCID 22841467 | 74% |
Reaktionsschritte
A mixture of 2-[2-aminoethoxymethyl]-4-(2-chlorophenyl)-3-ethoxycarbonyl-5-methoxycarbonyl-6-methyl-1,4-dihydropyridine (1.61 g), ("amlodipine"), (S)-4-benzyloxycarbonylamino-4-methoxycarbonylbutanoic acid (1.28 g) [see G. H. L. Nefkens and J. F. Nivard, Rec. Trav. Chim. Pays Bas, 199, 83, 1964], 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (0.83 g), 1-hydroxybenzotriazole (0.59 g) and triethylamine (0.44 g) in dichloromethane (25 ml) were reacted together as described in Example 5 part (a) to give the title compound (2.0 g) as an essentially pure solid foam which was used directly in Example 1 and Preparation 2 without further purification.
Herkunft & Nachweise
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patentnummer | US04806557 |
| Quelldatensatz | uspto-grants-1989_02 |
| ORD ID | ord-502a78c8ade34dfc9beb268d07f8c9fd |
| Quellennotiz | uspto-grants-1989_02 |