C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 263/16 (2006.01) A61K 31/4015 (2006.01) A61K 31/407 (2006.01) A61P 9/10 (2006.01) A61P 29/00 (2006.01) A61P 35/00 (2006.01) C07C 41/06 (2006.01) C07C 69/675 (2006.01) C07C 69/76 (2006.01) C07C 229/14 (2006.01) C07C 231/14 (2006.01) C07C 233/83 (2006.01) C07C 235/72 (2006.01) C07C 235/80 (2006.01) C07C 237/06 (2006.01) C07C 247/04 (2006.01) C07C 247/12 (2006.01) C07D 207/28 (2006.01) C07D 207/46 (2006.01) C07D 263/14 (2006.01) C07D 413/06 (2006.01) C07D 455/02 (2006.01) C07D 473/00 (2006.01) C07D 491/04
Patent
CA 2301054
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.
La présente invention a trait à une synthèse améliorée de clasto-lactacystine-.beta.-lactone et de ses analogues, dont la mise en oeuvre comporte moins d'étapes et permet d'obtenir des rendements globalement beaucoup plus élevés que les synthèses décrites dans les techniques actuelles. La voie de synthèse repose sur une nouvelle synthèse stéréospécifique d'un produit intermédiaire d'oxazoline, et sur une addition stéréosélective unique d'un amide formyle à l'oxazoline. L'invention concerne également de nouvelles clasto-lactacystine-.beta.-lactones et leurs analogues, ainsi que l'utilisation de ces composés comme inhibiteurs de protéasomes.
Behnke Mark
Plamondon Louis
Roush William
Soucy Francois
Behnke Mark
Mbm & Co.
Millennium Pharmaceuticals Inc.
Plamondon Louis
Roush William
LandOfFree
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