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Isolation, identification and synthesis of a metabolite of tazadolene succinate
W H Darlington1, D A Constable, L Baczynskyj
1Research Laboratories, Upjohn Limited, Crawley, UK.
Abstract:
Metabolism of tazadolene (1), a novel non-opioid analgesic with antidepressant properties, affords the 4-hydroxy and 3-methoxy-4-hydroxy derivatives (phenyl ring) of the drug, and N-[2-(phenylmethylene)cyclohexyl]-beta-alanine (4). The isolation, identification and synthesis of the latter metabolite is described.