Syntheses of Potential Metabolites of a Potent .KAPPA.-Opioid Receptor Agonist, TRK-820

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  • Syntheses of Potential Metabolites of a Potent κ-Opioid Receptor Agonist, TRK-820
  • Syntheses of Potential Metabolites of a Potent カッパ Opioid Receptor Agonist TRK 820

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Abstract

Chemical syntheses of three kinds of potential metabolites of TRK-820, a potent κ-opioid receptor agonist, were described. One of the potential metabolites 2, 17-N-dealkylated TRK-820, was synthesized starting from noroxycodone through 8 steps in 21% total yield. Glucuronidation of intermediate 10 and compound 1, the free base of TRK-820, was carried out stereoselectively to give 3-O-β-D-glucuronides 15 and 16 in good yields, respectively. Syntheses of potential conjugated metabolites 3 and 4 were accomplished through 10 steps and 2 steps in 11% and 43% total yields, respectively. Among the potential metabolites of TRK-820, compounds 2 and 4 were identified as metabolites in human hepatocytes. The results of pharmacological studies of compounds 2, 3, and 4 are described.

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