Access to 7 beta-analogs of codeine with mixed mu/delta agonist activity via 6,7-alpha-epoxide opening

作者：Magnus Philip; Ghavimi Bahman^*; Coe Jotham W

来源：Bioorganic & Medicinal Chemistry Letters, 2013, 23(17): 4870-4874.

DOI：10.1016/j.bmcl.2013.06.084

• Mixed mu/delta agonist
• Opioid
• Metopon
• 6,7-alpha-Epoxide

(-)-Codeine 1 was converted into previously unknown 7 beta-methyl-7,8-dihydrocodeine/morphine derivatives such as 13 via classical diaxial opening of alpha-epoxide 3. Several analogs exhibited dual mu/delta-agonist activity.

• 出版日期2013-9-1