Camptothecin derivatives and process for preparing same
US4473692A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Sep 1, 1982 |
| Grant date | Sep 25, 1984 |
| Priority date | — |
| Expiry date | Sep 1, 2002 |
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 is 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 is 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 a 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 a nitro group into the 10-positio…
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.