A diastereoselective synthesis of the title compound as a single E diastereomer has been efficiently accomplished by assembling the featured pyrano-indole scaffold of the spiro[cyclohexanedihydropyrano[ 3,4-b]-indole]-amine framework through an oxa-Pictet-Spengler reaction, promoted by a cheap and green Zeolite catalyst. Basic pharmacological experiments demonstrate that Cebranopadol acts as a mixed nociception/orphanin FQ (NOP) and mu (MOP) opioid receptor agonist useful for treatment of chronic pain.
A diastereoselective synthesis of Cebranopadol, a novel analgesic showing NOP/mu mixed agonism
FANTINATI, AnnaPrimo
;BIANCO, Sara;SALVADORI, Severo;PACIFICO, Salvatore;GUERRINI, Remo;CERLESI, Maria Camilla;TRAPELLA, Claudio
Ultimo
;CALO', Girolamo
2017
Abstract
A diastereoselective synthesis of the title compound as a single E diastereomer has been efficiently accomplished by assembling the featured pyrano-indole scaffold of the spiro[cyclohexanedihydropyrano[ 3,4-b]-indole]-amine framework through an oxa-Pictet-Spengler reaction, promoted by a cheap and green Zeolite catalyst. Basic pharmacological experiments demonstrate that Cebranopadol acts as a mixed nociception/orphanin FQ (NOP) and mu (MOP) opioid receptor agonist useful for treatment of chronic pain.File in questo prodotto:
| File | Dimensione | Formato | |
|---|---|---|---|
|
Fantinati_et_al-2017-Scientific_Reports.pdf
accesso aperto
Descrizione: Fantinati Scientific Report 2017
Tipologia:
Full text (versione editoriale)
Licenza:
Creative commons
Dimensione
1.72 MB
Formato
Adobe PDF
|
1.72 MB | Adobe PDF | Visualizza/Apri |
I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
