Enantioselective Total Synthesis of Fluvirucinin B₁

A convergent synthesis of fluvirucinin B₁ from acid <i>ent</i>-<b>6a</b> and nitrile <i>ent</i>-<b>9</b>, involving an organocopper coupling, a stereoselective allylation, a ring-closing metathesis reaction, and a stereoselective hydrogenation as the key steps, is reported. The starting building blocks have been prepared in a straightforward manner from a common phenylglycinol-derived lactam <b>1</b>. An unprecedented regioselective oxidation of phenylglycinol-derived secondary amines <b>5</b> to carboxylic acids <b>6</b> has been developed