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【结 构 式】 
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【药物名称】PNU-167532 【化学名称】2-Benzyl-4-(3,4-difluorophenyl)-4-oxobutyric acid 【CA登记号】 【 分 子 式 】C17H14Cl2O3 【 分 子 量 】337.20533 |
【开发单位】Pfizer (Originator) 【药理作用】Antiepileptic Drugs, Antiparkinsonian Drugs, Cerebrovascular Diseases, Treatment of, Cognition Disorders, Treatment of, Extrapyramidal Disorders, Treatment of, Ischemic Stroke, Treatment of, NEUROLOGIC DRUGS, Stroke, Treatment of, Kynurenine 3-Monooxygenase Inhibitors |
合成路线1
Conjugate addition of benzylmagnesium chloride (II) to unsaturated ketone (I) in the presence of cuprous iodide-dimethyl sulfide complex afforded the 2-benzyl derivative (III). Then, the ester function was saponified with NaOH in MeOH to give the title acid. Resolution of the enantiomers was effected by fractional crystallization of the ephedrine salts.
| 【1】 Giordani, A.; Pevarello, P.; Cini, M.; Bormetti, R.; Greco, F.; Toma, S.; Speciale, C.; Varasi, M.; 4-Phenyl-4-oxo-butanoic acid derivatives inhibitors of kynurenine 3-hydroxylase. Bioorg Med Chem Lett 1998, 8, 20, 2907. |