Synthesis of trans-2,6-Disubstituted Piperazines

Significance

A short and operationally simple synthesis of enantiopure trans-2,6-substituted piperazines is reported with excellent yields and high diastereoselectivity. Cyclization precursors 1 are readily available from chiral amino alcohols and simple allylamines by an improved practical protocol. The strategy takes advantage of the ­numerous established methods to prepare chiral amino alcohols.