Enantioselective Total Syntheses of (−)-FR901483 and (+)-8-<i>epi</i>-FR901483
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Abstract
The enantioselective total syntheses of the potent immunosuppressant
FR901483 (<b>1</b>) and its 8-epimer (<b>47</b>) have
been accomplished. Our approach features the use of building block <b>6</b> as the chiron, the application of the one-pot amide reductive
bis-alkylation method to construct the chiral aza-quaternary center
(dr = 9:1), regio- and diastereoselective intramolecular aldol reaction
to build the bridged ring, and RCM to form the 3-pyrrolin-2-one ring