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14-羟基二氢可待因酮(Oxycodone Ia)和14-羟基二氢吗啡酮(oxymorphinone)均为有效的镇痛药。最近Pasternak等报道14-羟基二氢吗啡酮腙(Ⅱa)为鸦片受体的不可逆结合激动剂,具有长效药理作用。我们曾合成了此化合物,发现它很不稳定,在乙醇溶液中放置后即分解,这与纳络酮与肼缩合制备纳络酮腙(Ⅱb)时为可逆反应的报道一致。为了增
Both Oxycodone Ia and oxymorphinone are potent analgesics. Recently, Pasternak et al. Reported that 14-hydroxyhydromorphone hydrazone (IIa) is an irreversible binding agonist of the opioid receptor and has long-lasting pharmacological effects. We have synthesized this compound and found it to be very unstable and decomposed after it was placed in ethanol. This is consistent with the report of reversible reaction of naloxone and hydrazine for the preparation of naloxone hydrazone (IIb). To increase