| 摘要 |
PURPOSE: A 2-methyl-4,9-dihydro-1- substituted-1h-imidazo£4,5-g| phthalazine-4,9-dione compound, a process for preparing the same compound and a pharmaceutical composition containing the same compound are provided, which compound has improved anticancer activity, so that it can be useful for prevention and treatment of various cancers. CONSTITUTION: The 2-methyl-4,9-dihydro-1- substituted-1h-imidazo£4,5-g| phthalazine-4,9-dione compound represented by formula (1) is provided, wherein R1 is hydrogen, methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, secondary butyl, tertiary butyl, n-pentyl, isopentyl, neopentyl, tertiary pentyl, 1-methylbutyl, 2-methylbutyl, 1,2-dimethylpropyl, n-hexyl, isohexyl, 1-methylpentyl, 2-methylpentyl, 3-methylpentyl, 1,1-dimethylbutyl, 1,2-dimethylbutyl, 2,2-dimethylbutyl, 1,3-dimethylbutyl, 2,3-dimethylbutyl, 3,3-dimethylbutyl, 1-ethylbutyl, 2-ethylbutyl, 1,1,2-trimethylpropyl, 1,2,2-trimethylpropyl, 1-ethyl-1-methypropyl, 1-ethyl-2-methylpropyl, phenyl, toluyl, xylyl or cumenyl. The process for preparing the 2-methyl-4,9-dihydro-1-substituted- 1h-imidazo£4,5-g|phthalazine-4,9-dione compound of formula (1) comprises the steps of: (i) reacting 6,7-dichloro-5,8-phthalazindione with sodium azide in a mole ratio of 1:1 to 1:4; (ii) reacting a reaction product of step (i) with sodium borohydride in a mole ratio of 1:0.5 to 1:1.5; (iii) reacting a reaction product of step (ii) with anhydrous acetate in the presence of concentrated sulfuric acid; (iv) reacting a reaction product of step (iii) with ammonia or amines in a mole ratio of 1:1 to 1:3; and (v) heating a reaction product of step (iv) with stirring.
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