3-烯-1,5-二炔是许多烯二炔类抗癌抗生素和发光材料的重要片断.发展了一种高选择性合成E-烯二炔化合物的两步法:(1)CuBr2为卤化剂,温和高效合成双卤代烯烃;(2)通过双卤代烯烃和末端炔烃的Sonogashira偶联反应构建烯二炔化合物.
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 enedivnes.