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EnglishA 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.
| Data di pubblicazione: | 2017 | |
| Titolo: | A diastereoselective synthesis of Cebranopadol, a novel analgesic showing NOP/mu mixed agonism | |
| Autori: | Fantinati, Anna; Bianco, Sara; Salvadori, Severo; Pacifico, Salvatore; Guerrini, Remo; Cerlesi, Maria Camilla; Trapella, Claudio; Calo', Girolamo | |
| Rivista: | SCIENTIFIC REPORTS | |
| Keywords: | Cebranopadol, Synthesis of Spiro compound | |
| Abstract in inglese: | 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. | |
| Digital Object Identifier (DOI): | 10.1038/s41598-017-02502-9 | |
| Handle: | http://hdl.handle.net/11392/2371408 | |
| Appare nelle tipologie: | 03.1 Articolo su rivista |
File in questo prodotto:
| File | Descrizione | Tipologia | Licenza | |
|---|---|---|---|---|
| Fantinati_et_al-2017-Scientific_Reports.pdf | Fantinati Scientific Report 2017 | Full text (versione editoriale) |  | Open Access Visualizza/Apri |
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