| 摘要 |
NEW MATERIAL:The heterocyclic compound derivative of formula I (R1 is group of formula II-IV; R2 is H or acyl; R3 is H, CH3 or NO2). EXAMPLE:1-(6'-Acetoxymethyl-2'-tetrahydropyranyl)-2-nitroimidazole. USE:A radiosensitizer for hypoxic cell. It has low toxicity and exhibits high sensitizing effect even at a low concentration. PREPARATION:A compound of formula I (R2=R4) can be produced by reacting a compound of formula V (R4 is acyl) with a compound of formula R1H preferably in an organic solvent such as ethyl acetate, acetonitrile, toluene, xylene, benzene, pyridine, triethylamine, etc., optionally in the presence of a reaction accelerator such as p-toluenesulfonic acid, anhydrous aluminum chloride, zinc chloride, anhydrous stannic chloride, hydrochloric acid, sulfuric acid, etc. The obtained compound can be converted to another compound of formula I (R2 is H) by conventional deacylation process.
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