Abstractmagnified imageThe new 7S‐aminolentiginosine has been synthesized by a diastereoselective 1,3‐dipolar cycloaddition strategy starting from 3,4‐dihydroxylated pyrroline N‐oxides derived from L‐tartaric acid in thirteen steps. The intermediate 7S‐azidolentiginosine undergoes efficiently copper(I)‐catalysed Huisgen cycloadditions to alkynes.