PURPOSE: The reaction of an alkali metal salt of 5-carboxyorotic acid with a halogenating reagent is followed by treatment of the product with an acid to give the titled compound, especially 5-iodoorotic acid, used as a medicine or its starting material, in high yield.
CONSTITUTION: A halogenating reagent is added as much, or in the form of an aqueous solution or solution in a inert organic solvent, to an aqueous solution of an alkali metal salt of 5-carboxyorotic acid of formulaI(M is Li, Na, K) and their reaction is effected by heating at 0W100°C and the resultant reaction product is acidified with a mineral acid at 0W30°C to give the objective compound. As a halogenating reagent, is used Br2, I2 or N-chlorosuccinimide. The compound of formulaIis obtained by making 3-amino-1,4-bis(alkoxycarbonyl) maleimide of formula III (R1, R2 are 1W4C alkyl) react with an alkali hydroxide in water at room temperature or under heating and acidifying the reaction mixture with a mineral acid.
KITA JIYUNICHIROU
KAKEYA NOBORU
YOKOO YASUHIKO
