| 摘要 |
PURPOSE: A novel process prepares N-(amino-4,6-dihalogenopyrimidine)formamides (formula 1 and 2) at high yields from the reaction of 2,5-diamino-4,6-dihalogenopyrimidine(formula 3) with formic acid. CONSTITUTION: 2,5-diamino-4,6-dihydroxypyrimidine(formula 4) or salt thereof is reacted with halogenated hydrocarbon in the presence of phosphorus oxychloride and tertiary ammonium halide or amine to afford 2,5-diamino-4,6-dihalogenopyrimidine(formula 3) at a high yield. Then, the 2,5-diamino-4,6-dihalogenopyrimidine, preferably 2,5-diamino-4,6-dihalogenopyrimidine or 2,5-diamino-4,6-dibromopyrimidine, is reacted with formic acid and directly converted to N-(amino-4,6-dihalopyrimidine)formamide(formula 1 or 2). Specifically, in the process for preparing compounds of formula 1, the reaction is carried out at temperatures of 20 to 60°C, preferably 25 to 55°C using 70-80% of formic acid. On the other hand, in the process for preparing compounds of formula 2, the reaction is carried out at temperatures of 0 to 30°C, preferably 10 to 25°C using 80-98% of formic acid.
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