Tubulysin V has been enantioselectively synthesized from the units of dipeptide 23, Tuv and
Tup. The features of this synthetic strategy is included three portions, the Tuv fragment 17 was
disasteroselectively synthesized from the D-malic acid, the stereocenters of the Tup unit was
constructed by the asymmetric reduction as well as methylation, and the epimerization for
several known methods was successfully avoided by condensation of fragment 19 with 24, and
by deprotection with hydrogenation.