| abstract |
"SYNTHESIS OF CLASTO-LACTACISTINA <225> -LACTONA ESEUS ANALOGUE". The present invention is directed to an improved synthesis of clasto-lactacistin- <225> -lactone, and its analogs, which proceeds in fewer steps and in a much higher overall yield than syntheses described in the prior art. The synthetic pathway is based on a new stereospecific synthesis of an oxazoline intermediate and a unique stereoselective addition of a formyl amide to oxazoline. New clasto-lactacistin- <225-lactones and their analogues and their use as proteasome inhibitors are also described. |