Synthesis of clasto-lactacystin .beta.-lactone and analogs thereof
US6294560A · kind A · utility
54Cited by
1References
6Claims
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Assignee
Inventors
Key dates
| Filing date | Jun 20, 2000 |
| Grant date | Sep 25, 2001 |
| Priority date | — |
| Expiry date | Jun 20, 2020 |
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-.beta.-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-.beta.-lactones, and analogs thereof and their use as proteosome inhibitors.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.