Synthesis of clasto-lactacystin &bgr;-lactone and analogs thereof
US6566553B2 · kind B2 · utility
27Cited by
4References
2Claims
0Family size
Assignee
Inventors
Key dates
| Filing date | Aug 10, 2001 |
| Grant date | May 20, 2003 |
| Priority date | — |
| Expiry date | Aug 10, 2021 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07B2200/07
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
The present invention is directed to an improved synthesis of clasto-lactacystin-&bgr;-lactone, and analogs thereof, that proceeds in fewer steps and in much greater overall yield than syntheses described in the prior art. The synthetic pathway relies upon a novel stereospecific synthesis of an oxazoline intermediate and a unique stereoselective addition of a formyl amide to the oxazoline. Also described are novel clasto-lactacystin-&bgr;-lactones, and analogs thereof and their use as proteosome inhibitors.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.