(e)-5-(2-bromovinyl)-uridine, its derivatives and a process...

C - Chemistry – Metallurgy – 07 – H

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204/91.17, 260/2

C07H 19/067 (2006.01) C07H 19/06 (2006.01)

Patent

CA 1207760

A b s t r a c t o f t h e d i s c l o s u r e The invention relates to (E)-5-(2-bromo- vinyl)-uridine and its derivatives of general formula (VI) Image (VI) wherein R1 stands for a hydrogen atom, C1-8 alkanoyl group, benzoyl group or a benzoyl group substituted in para position either with a C1-4 alkyl group or a halogen atom, and a process for preparing them by brominating 2',3',5'-tri-0-acyl-5-ethyl-uridine of general formula (IV) Image (IV) - 2 - wherein R is identical with R1, except where R1 stands for a hydrogen atom, dehydrohalogenating the resulting dibromo compound of general formula (V) Image (V) 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.

410918

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