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【结 构 式】

【药物名称】Palatrigine, BW A256C

【化学名称】5(3)-Amino-6-(2,3-dichlorophenyl)-2,3(2,5)-dihydro-3(5)-imino-2-isopropyl-1,2,4-triazine

【CA登记号】98410-36-7, 98410-66-3 (monoHI), 98410-37-8 (monomethanesulfonate)

【 分 子 式 】C12H13Cl2N5

【 分 子 量 】298.17691

【开发单位】GlaxoSmithKline (Originator)

【药理作用】Antiarrhythmic Drugs, CARDIOVASCULAR DRUGS

合成路线1

3,5-Diamino-6-(2,3-dichlorophenyl)-1,2,4-triazine (lamotrigine) (I) is alkylated with 2-iodopropane in refluxing pentan-2-one. The free base, obtained following treatment of the hydroiodide with methanolic sodium hydroxide, is converted to the title compound with methanolic hydrogen chloride.

1 Miller, A.A.; Allan, G.; Sawyer, D.A. (Glaxo Wellcome plc); 1,2,4-Triazines. EP 0142306; ES 8606304; JP 1985109577; US 4649139 .
2 Donoghue, S.; Sawyer, D.; Allan, G.; BW-A256C. Drugs Fut 1987, 12, 7, 621.
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) 28842 3-amino-6-(2,3-dichlorophenyl)-1,2,4-triazin-5-ylamine C9H7Cl2N5 详情 详情
(II) 19369 2-iodopropane 75-30-9 C3H7I 详情 详情
(III) 28843 3-amino-6-(2,3-dichlorophenyl)-2-isopropyl-2,3-dihydro-1,2,4-triazin-5-ylamine C12H13Cl2N5 详情 详情
Extended Information