Diastereoselective Synthesis of Functionalized Diketopiperazines through Post-transformational Reactions.

A diversity-oriented access to diastereoselective arylidene 2,5-diketopiperazines is elaborated via a sequential Ugi post-transformation involving catalytic cyclization and oxidative Heck reaction sequence. This sequence offers an interesting multicomponent entry to a library of 2,5-diketopiperazines and arylidene 2,5-diketopiperazines under mild reaction conditions in good to excellent yields.