Towards immunoproteasome-specific inhibitors: An improved synthesis of dihydroeponemycin

Eponemycin, an antitumor and antiangiogenic epoxy ketone natural product, is previously shown to target proteasome for its activity. Although there have been many synthetic approaches developed, practical and efficient synthetic strategy for eponemycin has yet to be accomplished. Here, we report an efficient new route for the preparation of dihydroeponemycin, an active eponemycin derivative. This will aid the design of proteasome inhibitors with novel activity.