abstract |
A process for the preparation of a compound of a formula (I), wherein R1 and R2, which may be the same or different, represent aliphatic, araliphatic or aryl groups, and R represents a group -CH2CH(OCONH2)-CH2OX in which X is a C1-5 alkyl group, which comprises reacting a compound of formula (II), wherein R1 and R2 and X are as defined above with a dihalophosphinyl or halosulphonyl isocyanate to obtain a compound of formula (III), wherein R1 and R2 and X are as defined above and Z is a group of formula -SO2Y or -POY2 wherein Y is a halogen atom followed by hydrolysis of the compound of formula (III) is described. Also described are several N-dihydroxyphosphoryl pyrimidinetrione derivatives which are intermediates in the above process, some of which may also be useful as water soluble prodrugs of certain pyrimidinetrione compounds. |