HuagongsheHuagongshe Chemie-Druckbericht · Nur für Forschungszwecke
Triethylamine → Dicyclohexylcarbodiimide
Beteiligte Stoffe
| Rolle | Name | HCID | Einwaage |
|---|---|---|---|
| Edukt | Triethylamine | HCID 8471 | — |
| Edukt | 1-Hydroxybenzotriazole | HCID 75771 | — |
| Edukt | Perindopril Erbumine | HCID 441313 | — |
| Edukt | (2S)-2-[[(2S)-1-ethoxy-1-oxopentan-2-yl]amino]propanoic acid | HCID 10015159 | — |
| Edukt | (2S,3aS,7aS)-2-carboxyperhydroindole, p-toluenesulfonate salt | HCID 131727202 | — |
| Produkt | Dicyclohexylcarbodiimide | HCID 10868 | — |
Reaktionsschritte
WO 01/58868 discloses a method for preparation of perindopril erbumine comprising reacting benzyl ester of (2S,3aS,7aS)-2-carboxyperhydroindole, p-toluenesulfonate salt with (S,S) diastereoisomer of N-[(S)-1-carbethoxybutyl]-(S)-alanine in the presence of 0.4 to 0.6 moles of 1-hydroxybenzotriazole; 1 to 1.2 moles of dicyclohexylcarbodiimide and 1 mole of triethylamine at 77° C. to give the dipeptide compound, which on debenzylation gives perindopril.
Herkunft & Nachweise
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patentnummer | US07456296B2 |
| Quelldatensatz | uspto-grants-2008_11 |
| ORD ID | ord-d19c382cafa745abb9ff8c511491009a |
| Quellennotiz | uspto-grants-2008_11 |