α-Cyanation of N-protected cyclic amines was achieved using a direct electrochemical method. Unsubstituted N-protected cyclic amines were easily cyanated at the α-position using an undivided cell in high yields; moreover, α-cyanation of αâ²-substituted pyrrolidine and αâ²-,βâ²- or γ-substituted piperidines smoothly proceeded in high yield and with high to excellent diastereoselectivity. α-Substituted N-cyano-pyrrolidines and -piperidines were also cyanated at the more substituted position (the α-position) using a divided cell with high yield and high regioselectivity.
通过直接电
化学方法,实现了N-保护的环状胺的α-
氰化。未取代的N-保护环状胺在无隔膜电池中易于在α位进行
氰化,产率很高;此外,α'-取代的
吡咯烷和α'、β'或γ-取代的
哌啶也能顺利进行高产率的α-
氰化,并具有高度至优异的非对映选择性。α-取代的N-
氰基
吡咯烷和
哌啶在有隔膜电池中也能在更取代的位置(α位)进行
氰化,产率高且具有高区域选择性。