Conversion of uracil derivatives to cytosine derivatives
US4754026A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | May 27, 1986 |
| Grant date | Jun 28, 1988 |
| Priority date | — |
| Expiry date | May 27, 2006 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07H19/06
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
A process is disclosed for producing a 4-O-sulfonyluracil derivative of the formula ##STR1## [wherein R.sup.1 is hydrogen, halogen, alkyl and alkoxy, R.sup.2 is glycosyl having protected hydroxyls; and --SO.sub.2 R.sup.3 is an organic sulfonyl] which comprises reacting an uracil derivative of the formula ##STR2## [wherein R.sup.1 and R.sup.2 are as defined above] with an organic sulfonylating agent of the formula R.sup.3 SO.sub.2 X [wherein R.sup.3 SO.sub.2 is an organic sulfonyl and X is halogen] in the presence of potassium carbonate. The obtained 4-O-sulfonyluracil is further subjected to amination. The processes are industrially adavantageous and produce cytosine derivatives such as cytidine in high yield.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.