Photochemical process for preparing camptothecin derivatives
US4545880A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Jul 18, 1984 |
| Grant date | Oct 8, 1985 |
| Priority date | — |
| Expiry date | Jul 18, 2004 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D491/22
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
New Camptothecin derivatives possessing high anti-tumor activity with slight toxicity, represented by the general formula: ##STR1## wherein R.sup.1 stands for a hydrogen atom, an alkyl group, a hydroxyl group, an alkoxy group or an acyloxy group, R.sup.2 for a hydrogen atom, an alkyl group, an aralkyl group, a hydroxymethyl group, a carboxymethyl group or an acyloxymethyl group, and R.sup.3 for the grouping --XR' (where R' is a hydrogen atom, an alkyl group or an acyl group and X is an oxygen atom or a sulfur atom), a nitro group, an amino group, an alkylamino group, an acylamino group or a halogen atom, with the proviso that when both of R.sup.1 and R.sup.2 are hydrogen atoms, R.sup.3 should not be hydroxyl group, methoxy group or acetoxy group. These new camptothecin derivatives are prepared by treating a 5-R.sup.1 -7-R.sup.2 camptothecin derivative with a peroxidant and then reacting the resultant 5-R.sup.1 -7-R.sup.2 -camptothecin-1-oxide with an active hydrogen compound under irradiation of UV-rays or by catalytically hydrogenating the ring B of camptothecin in a solvent, treating the resultant tetrahydro product with an acylating agent, introducing nitro group into 10-positio…
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.