Process for producing 5-fluorouracil and derivatives thereof in acid and/or alcohol solvents
US4029661A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Jul 13, 1972 |
| Grant date | Jun 14, 1977 |
| Priority date | — |
| Expiry date | Jul 13, 1992 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D239/22
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
Direct fluorination of uracil, cytosine and their derivatives, in the presence of a non-aqueous solvent, by fluorine gas to produce 5-fluorouracil, 5-fluorocytosine, 5-fluorouracil derivatives and 5-fluorocytosine derivatives is disclosed. The non-aqueous solvent is an acid or alcohol, which can be partly or fully fluorinated or chlorinated, of up to 8 carbon atoms, such as trifluoroacetic acid. Novel compounds produced by the reaction, such as 5,5-difluoro-5,6-dihydro-6-(2,2,2-trifluoroethoxy) uracil are also disclosed. The derivatives and 5-fluorocytosine are useful as germicidal and antineoplastic agents while 5-fluorouracil itself is a known cancer chemotherapy agent.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.