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:
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Fantinati_et_al-2017-Scientific_Reports.pdf
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Descrizione: Fantinati Scientific Report 2017
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