Process for preparing pyrimidinetrione derivatives

Details Process for preparing pyrimidinetrione derivatives Process for preparing pyrimidinetrione derivatives

C - Chemistry, Metallurgy

07

D

260/256

C07D 239/62 (2006.01)

Patent

CA 1247619

Abstract A process for the preparation of pyrimidinetrione derivatives of formula (I) is described Image (I) wherein R1 and R2, which may be the same or different, represent aliphatic, araliphatic or aryl groups, and R3 represents a group of the formula -CH2CH(OCONH2)- CH2OX wherein X is hydrogen or a C1-5 alkyl group which comprises reacting approximately equimolar amounts of a monoalkali metal salt of a compound of formula (I), wherein R3 is a hydrogen atom, with an alkylating agent R3Hal wherein R3 is as defined above and Hal represents a halogen atom, in the presence of at least 0.2 moles of an acid of formula (I) wherein R3 is a hydrogen atom per mole of alkali metal salt. The yield is increased by up to 50% by this method. The process is of particular application to the preparation of febarbamate, 1-(3-nbutoxy-2-carbamoyloxypropyl)- 5-ethyl-5-phenyl-(1H,3H,5H)pyrimidlne-2,4,6-trione. Also described is a method of treating geriatrics using febarbamate which has particular advantages in reducing irritability and antisocial behaviour.

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