| 摘要 |
An improved process of producing known 5-pyrimidine carboxylic acids which have in 4-position a basic group, such as the 2,3-dimethyl anilino, 3-trifluoro methyl anilino, dimethylamino, anilino, N-methyl anilino, and other groups, by using the readily available malonic acid dinitrile or dimethylamino methylene malonic acid dinitrile and dimethylformamide chloride as starting reactants, reacting said reactants at a temperature between 10 DEG C. and 110 DEG C., preferably in the presence of an inert solvent to yield the heretofore unknown 1-dimethylamino-3-chloro-4-cyano-2-azapentadiene-5-dimethyliminium chloride which is preferably purified by conversion into the perchlorate, replacing the chlorine atom in 3-position by an amino group to yield the heretofore unknown corresponding 1-amino-1-dimethylamino methylene amino-3-dimethyliminium-2-cyano propene-(1) compound, causing ring closure to the corresponding 4-amino-5-cyano pyrimidine compound by reaction with ammonia, and saponifying the cyano group to the carboxyl group. The final products are known antiphlogistic, analgesic, and antirheumatic drugs.
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