Abstract: This invention relates to a process for preparation of pyrimidinetriones. It also relates to novel N-dihydroxyphosphoryl pyrimidinetrione derivatives which may be useful as water-soluble prodrugs of certain pyrimidinetrione compounds.
Type:
Grant
Filed:
October 30, 1991
Date of Patent:
November 16, 1993
Assignee:
Sapos S.A.
Inventors:
Bernard Siegfried, Jindrich Vachta, Karel Valter, Stephane Hugentobler
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.
Type:
Grant
Filed:
April 11, 1984
Date of Patent:
September 9, 1986
Assignee:
Sapos S.A.
Inventors:
Philippe Gold-Aubert, Diran Melkonian, Jindrich Vachta, Karel Valter, Bernard Siegfried, Stephane Hugentobler
Abstract: Discrete tetrameric complexes of malonylurea derivatives are described in which the properties expected of the individual malonylurea derivatives are beneficially modified. The complexes are of high purity and are of considerable value in the treatment of alcoholism. Simple processes for preparing the complexes are also disclosed as are compositions containing them.