Synthesis of clasto-lactacystin .beta.-lactone and analogs thereof

   
   

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 proteasome inhibitors.

Присытствыющий вымысел направлен к улучшенному синтезу clasto-lactacystin-.beta.-lactone, и аналогам thereof, которые выручки в немногих шагах и в очень большом общем выходе чем синтезы описали в прежнем искусствое. Синтетический pathway полагается на синтезе романа stereospecific оксазолина промежуточного и уникально stereoselective добавлении амида формила к оксазолину. Также описаны роман clasto-lactacystin-.beta.-lactones, и аналоги thereof и их польза как proteasome иы АБС битор.

 
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