Organic compounds -- part of the class 532-570 series – Organic compounds – Nitrogen attached directly or indirectly to the purine ring...
Patent
1984-04-11
1986-09-09
Daus, Donald G.
Organic compounds -- part of the class 532-570 series
Organic compounds
Nitrogen attached directly or indirectly to the purine ring...
C07D23962
Patent
active
046110577
ABSTRACT:
A process for the preparation of pyrimidinetrione derivatives of formula (I) is described ##STR1## wherein R.sup.1 and R.sup.2, which may be the same or different, represent aliphatic, araliphatic or aryl groups, and R.sup.3 represents a group of the formula --CH.sub.2 CH(OCONH.sub.2)--CH.sub.2 OX wherein X is hydrogen or a C.sub.1-5 alkyl group which comprises reacting approximately equimolar amounts of a monoalkali metal salt of a compound of formula (I), wherein R.sup.3 is a hydrogen atom, with an alkylating agent R.sup.3 Hal wherein R.sup.3 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 R.sup.3 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-.sup.n butoxy-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.
REFERENCES:
patent: 3075983 (1963-01-01), Gold-Aubert
Gold-Aubert et al., Helvetica Chimica Acta, XLIV, pp. 105-113 (1960).
Gold-Aubert Philippe
Hugentobler Stephane
Melkonian Diran
Siegfried Bernard
Vachta Jindrich
Daus Donald G.
Kapner Stephen M.
Sapos S.A.
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