Formal Total Synthesis of (+)-Gephyrotoxin

An efficient formal total synthesis of (+)-gephyrotoxin is described. The key step of our strategy relies on the diastereoselective reduction of a chiral pyrrolidine β-enamino ester obtained by condensation of (<i>S</i>)-phenylglycinol on a protected 8-hydroxy-3,6-dioxooctanoate.