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55FLUOROO66HYDROXYY66CARBOXYY5*66DIHYDROOURACIL AND ITS PREPARATION

机译:55FLUOROO66HYDROXYY66CARBOXYY5 * 66双氢尿酸及其制备方法

摘要

NEW MATERIAL:5-FLUORO-6-hydroxy-6-carboxy-5,6-dihydrouracil expressed by the formula. USE:An intermediate for a fluorine-containing compound, e.g.5-fluorouracil, etc., useful as an anti-tumor agent. PREPARATION:A desired compound is prepared by reacting orotic acid with fluorine gas in the presence of water. Preferably the reaction is carried out in formic acid containing 5-20 wt.% of water as a solvent at 5-50 deg.C. Orotic acid-hydrate is advantageously used as the acid source due to its high availability, etc., and fluorine gas is preferably diluted with an inert gas. Fluorine gas may be replaced by trifluoromethylhypofluorite. The desired compound can be easily separated from the unreacted materials with water, and thermal treatment of the aqueous solution at = 130 deg.C easily gives 5-fluorouracil.
机译:新材料:由式表示的5-氟6-羟基-6-羧基-5,6-二氢尿嘧啶。用途:含氟化合物的中间体,例如5-氟尿嘧啶等,可用作抗肿瘤剂。制备:所需的化合物是通过使乳清酸与氟气在水存在下反应制备的。优选地,反应在5-50℃下在含有5-20重量%的水作为溶剂的甲酸中进行。乳清酸水合物由于其高可用性等而有利地用作酸源,并且氟气优选地用惰性气体稀释。氟气可用三氟甲基次萤石代替。可以容易地用水将期望的化合物与未反应的物质分离,并且在≥130℃下对水溶液进行热处理容易得到5-氟尿嘧啶。

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