Beschreibung:
<jats:title>Abstract</jats:title><jats:p>The total synthesis of tubulysin V was accomplished in 1.0% overall yield with linear 13 steps. Our synthetic strategy featured the following two reactions. One is zinc‐mediated aza‐Barbier reaction of (<jats:italic>R</jats:italic>)‐<jats:italic>N</jats:italic>‐<jats:italic>tert</jats:italic>‐butanesulfinyl imine <jats:bold>8</jats:bold> with <jats:italic>β</jats:italic>‐ester group functionalized allylic bromide <jats:bold>9</jats:bold> to afford the chiral homo‐allylic amine (<jats:bold>7</jats:bold>); the other is to employ the methodology of aqueous indium‐mediated aza‐Barbier reaction previously developed by our group, giving the chiral homo‐allylic amine <jats:bold>13</jats:bold> with high efficiency.</jats:p>