Process for the preparation of 5-(2-bromovinyl)-uridine
US4544740A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Sep 7, 1982 |
| Grant date | Oct 1, 1985 |
| Priority date | — |
| Expiry date | Sep 7, 2002 |
Classification
- Technology area (CPC A)Human Necessities
- CPC primaryA61P31/12
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
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.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.