摘要

3-Ene-1,5-diyne was a key building block found in many enediyne antitumor agents and designed materials. A stereocontrolled route to synthesize E-enediynes was developed, which included the following two steps: (1) a mild and economical method to synthesize dihalo vinyl derivatives via the addition of CuBr2 to alkyne, and (2) the Sonogashira coupling reaction of dihalo vinyl and terminal alkynes to conjugated enediynes.