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【结 构 式】 
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【药物名称】Nalmetrene(former INN; USAN), Nalmefene, NIH-10365(HCl), ORF-11676, JF-1, Cessal, Soberal, Alcofene, Revex(HCl), Arthene, Cervene, Incystene 【化学名称】N-(Cyclopropylmethyl)-4,5alpha-epoxy-6-methylenemorphinan-3,14beta-diol 【CA登记号】55096-26-9 【 分 子 式 】C21H25NO3 【 分 子 量 】339.4383 |
【开发单位】Baker Norton (Originator), BioTie Therapies (Not Determined), Baxter (Licensee), SSP (Licensee) 【药理作用】Antagonists to Narcotics, Antipsychotic Drugs, Cerebrovascular Diseases, Treatment of, NEUROLOGIC DRUGS, PSYCHOPHARMACOLOGIC DRUGS, Specific Antidotes, Stroke, Treatment of, Treatment of Alcohol Dependency, TREATMENT OF POISONING, DRUG ABUSE & DEPENDENCY, Treatment of Substance Dependency, kappa-Opioid Antagonists |
合成路线1
By a Wittig reaction at naltrexone (I) with triphenylmethylphosphonium bromide (II) in DMSO by means of NaH as base.
| 【1】 Hahn, E.F.; Fishman, J.; Narcotic antagonists. 4. Carbon-6 derivatives of N-substituted noroxymorphones as narcotic antagonists. J Med Chem 1975, 18, 3, 259-262. |
| 【2】 Hermann, E.C.; Lee, K.T.; Myers, M.J. (DuPont Pharmaceuticals Co.); 17-Substituted-6-desoxy-7,8-dihydro-6alpha-methylnoroxymorphone narcotic antagonists. EP 0039066; JP 167687; US 4322426 . |
| 【3】 Serradell, M.N.; Castaner, J.; Nalmefene. Drugs Fut 1984, 9, 7, 518. |