Process for the preparation of 9-amino camptothecin
US5614628A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Sep 28, 1994 |
| Grant date | Mar 25, 1997 |
| Priority date | — |
| Expiry date | Sep 28, 2014 |
Classification
- Technology area (CPC F)Mechanical Engineering; Lighting; Heating
- CPC primaryF23C5/02
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
A process for preparing 9-amino camptothecin comprising the steps of: (1) reacting a compound of formula (III) ##STR1## wherein the hydroxy group on ring A is in the 10- or 12-position, with a nitrating agent, to form the corresponding 9-nitro compound; (2) converting the 9-nitro compound into a corresponding compound of formula (V) ##STR2## wherein XO is a group that can be removed reductively; and (3) reductively removing the XO group and reducing the nitro group of the compound of formula (V), to form the 9-amino camptothecin, a known antitumor compound. The present invention also includes compound having the above formula (V) and their 9-amino analogs, which have antitumor activity.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.