HuagongsheHuagongshe Chemie-Druckbericht · Nur für Forschungszwecke
Hydrochloric Acid → 2-Aminopyridinoyl-piperidine
Beteiligte Stoffe
| Rolle | Name | HCID | Einwaage |
|---|---|---|---|
| Edukt | Hydrochloric Acid | HCID 313 | — |
| Edukt | Benzophenone imine | HCID 136809 | — |
| Edukt | Binap, (A+-)- | HCID 634876 | — |
| Edukt | Sodium t-butoxide | HCID 23676156 | — |
| Edukt | 2-Chloropyridinoyl-piperidine | HCID 67442558 | — |
| Lösungsmittel | Toluene | HCID 1140 | — |
| Lösungsmittel | Tetrahydrofuran | HCID 8028 | — |
| Produkt | 2-Aminopyridinoyl-piperidine | HCID 67443361 | — |
Reaktionsschritte
Next, the 2-chloropyridinoyl-piperidine intermediate is reacted with benzophenone imine in the presence of tris(dibenzylidineacetone)-dipalladium(0) Pd2(dba)3) as a catalyst, and 2,2′-bis(diphenylphosphino)-1,1′-binaphthyl (BINAP) and sodium t-butoxide in a suitable solvent, such as toluene, at reflux, to substitute the halo group with the benzophenone imino group. After work-up, this intermediate is typically reacted with hydrochloric acid in a suitable solvent, such as tetrahydrofuran, and then purified to give the corresponding 2-aminopyridinoyl-piperidine intermediate.
Herkunft & Nachweise
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patentnummer | US07423050B2 |
| Quelldatensatz | uspto-grants-2008_09 |
| ORD ID | ord-9b02042daf3a4b20971170c5f1a9a16c |
| Quellennotiz | uspto-grants-2008_09 |