Loading patent…
AssigneeEgyt Gyogyszervegyeszeti Gyar
InventorsAnna Szabolcs nee Borbas, Laszlo tvos, Janos Sagi, Attila Szemzo, Maria Peredy nee Kajtar, Istvan Horvath, Istvan Koczka, Csilla Rethati, Pal Ivan, Ildiko Fritzsche nee Lukacs, Janos Nagy
Estimating the term…
The invention relates to (E)-5-(2-bromovinyl)-uridine and its derivatives of general formula VI, ##STR1## wherein R.sup.1 stands for a hydrogen atom, C.sub.1-8 alkanoyl group, benzoyl group or a benzoyl group substituted in para position either with a C.sub.1-4 alkyl group or a halogen atom, and a process for preparing them by brominating 2',3',5'-tri-O-acyl-5-ethyl-uridine of general formula IV, ##STR2## wherein R is identical with R.sup.1, except where R.sup.1 stands for a hydrogen atom, dehydrohalogenating the resulting dibromo compound of general formula V ##STR3## and optionally deacylating it. The resulting compounds of general formula VI are exhibiting significant potency against Herpes simplex virus species and are of remarkably low acute toxicity.
A process for the preparation of (E)-5-(2-bromovinyl)-uridine and its derivatives of formula VI, ##STR6## wherein R.sup.1 stands for hydrogen, C.sub.1-8 alkanoyl, benzoyl or benzoyl substituted in the para position either with C.sub.1-4 alkyl or halogen, by brominating 2',3',5'-tri-O-acyl-5-ethyl-uridine of formula IV, ##STR7## wherein R is identical with R.sup.1 as defined above, except where R.sup.1 stands for a hydrogen atom, with bromine,--dehydrohalogenating the resulting dibromo compound of formula V, ##STR8## wherein R is identical with R.sup.1 as defined above, except where R.sup.1 stands for hydrogen.
Dependencies are inferred from the claim text.