Abstract

A 19-step synthesis of (±)-cribrostatin 4 ( 1) from readily available piperazine-2,5-dione derivative 6 is described. The synthesis features the concise construction of a pentacyclic framework, followed by the base-catalyzed epimerization of the C-1 stereo center of aldehyde ( 11). The results of cytotoxicity studies are also presented.

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