| 摘要 |
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)pyrimidine-2,4,6-trione. Also described is a method of treating geriatrics using febarbamate which has particular advantages in reducing irritability and antisocial behavior. |
