Synthesis of phenstatin and prodrugs thereof
US6943194B1 · kind B1 · utility
4Cited by
2References
6Claims
0Family size
Assignee
Inventors
Key dates
| Filing date | Jan 9, 1999 |
| Grant date | Sep 13, 2005 |
| Priority date | — |
| Expiry date | Jan 9, 2019 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07F9/12
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
A newly discovered antineoplastic compound denominated “phenstatin” is herein described as are synthetic methods for producing phenstatin and the active prodrug thereof. Phenstatin was converted to the sodium phosphate prodrug (3d) by a dibenzylphosphite phosphorylation and subsequent hydrogenolysis sequence 3b→3c→3d. Phenstatin (3b) was found to be a potent inhibitor of tubulin polymerization and the binding of colchicine to tubulin comparable to combretastatin A-4 (1b).
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.