Abstract: Azetidine-2-carboxylic acid (Aze) is an extremely interesting and promising molecule in terms of its structure and application in organic synthesis. Aze is widely used in the synthesis of various peptides and phytosiderophores, as well as in coordination chemistry and catalysis. This review for the first time summarizes and examines the results of diverse studies related to the use of Aze and its derivatives in organic synthesis.