Process for the preparation of taxane derivatives and .beta.-lactam intermediates therefor
US6218553A · kind A · utility
Assignee
Inventor
Key dates
| Filing date | Feb 29, 2000 |
| Grant date | Apr 17, 2001 |
| Priority date | — |
| Expiry date | Feb 29, 2020 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D205/08
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
Taxol (I) is a complex deterpene which is currently considered the most exciting lead in cancer chemotherapy. Taxol possesses high cytotoxicity and strong antitumor activity against different cancers which have not been effectively treated by existing antitumor drugs. However, taxol has a problem with solubility in aqueous media, which may impose some serious limitation in its use. Taxotere (III) seems to have antitumor activity superior to taxol with better bioavailability. Taxotere has a modified taxol structure with a modified C-13 side chain. This fact strongly indicates that modification on the C-13 side chain would provide a new series of taxol and Taxotere analogues which may have higher potency, better bioavailability and less unwanted toxicity. The present invention provides efficient and practical methods for the syntheses of Taxotere and its analogues through .beta.-lactam intermediates and their coupling with baccatin III.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.