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 5W20 wt.% of water as a solvent at 5W50°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°C easily gives 5-fluorouracil.
UCHIDA KEIICHI
MORIKAWA SHINSUKE
NOSHIRO MAKOTO
