An asymmetric synthesis of the tubulin polymerisation inhibitor (S)-(−)-N-acetylcolchinol is reported based on an intramolecular biaryl oxidative coupling of a 1, 3-diarylpropyl acetamide intermediate using phenyliodonium bis (trifluoroacetate) as the final step. Three syntheses of the penultimate 1, 3-diarylpropyl acetamide intermediate (S)-(−)-N-[1-[3-(tert- butyldimethylsilyloxy) phenyl)]-3-(3, 4, 5-trimethoxyphenyl) propyl] acetamide are ...