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【结 构 式】

【药物名称】Deferiprone, CP20, CGP-37391, CP020, L1, Ferriprox, Deferum, Kelfer

【化学名称】3-Hydroxy-1,2-dimethyl-4(1H)-pyridone

【CA登记号】30652-11-0

【 分 子 式 】C7H9NO2

【 分 子 量 】139.15528

【开发单位】BTG (Technology Transfer), Cipla (Originator), Royal Free Hospital (Originator), Chiesi (Not Determined), Apotex (Licensee), Cangene (Licensee)

【药理作用】Antagonists to Metals, Specific Antidotes, TREATMENT OF POISONING, DRUG ABUSE & DEPENDENCY, Metal Chelators

合成路线1

A new synthesis of L1 has been reported: The reaction of 3-benzyloxy-2-methyl-4H-pyran-4-one (I) with methylamine and NaOH in refluxing ethanol gives 3-benzyloxy-1,2-dimethylpyridin-4(1H)-one (II), which is deprotected by hydrogenolysis with H2 over Pd/C in ethanol.

1 Dobbin, P.S.; Hider, R.C.; Porter, J.B.; Sarpong, P.; Hall, A.D.; Xiao, G.; Taylor, P.D.; Van der Helm, D.; Synthesis, physicochemical properties, and biological evaluation of N-substituted 2-alkyl-3-hydroxy-4(1H)-pyridinones: Orally active iron chelators with clinical potential. J Med Chem 1993, 36, 17, 2448.
中间体序号 中间体编号 品名 CAS号 分子式 供应商 用于合成
(I) 12074 3-(Benzyloxy)-2-methyl-4H-pyran-4-one;3-(benzyloxy)-2-methylpyran-4-one 61049-69-2 C13H12O3 详情 详情
(II) 12075 3-(Benzyloxy)-1,2-dimethyl-4(1H)-pyridinone C14H15NO2 详情 详情
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