A Total Synthesis of Salinosporamide A.

Marx LB, Burton JW

Salinosporamide A is a β-lactone proteasome inhibitor currently in clinical trials for the treatment of multiple-myeloma. Herein we report a short synthesis of this small, highly functionalized, biologically important natural product that uses an oxidative radical cyclization as a key step and allows for the preparation of gram quantities of advanced synthetic intermediates.

Keywords:

Free Radicals

,

Lactones

,

Pyrroles

,

Biological Products

,

Cyclization

,

Oxidation-Reduction

,

Proteasome Inhibitors