Macrocyclic compounds are of growing interest because of thei matural existence, their interesting biological, physicochemical properties, and potential applications in medicine. Various natural as well as non-natural macrocycles have been synthesized, and synthetic methodologies aiming to access macrocycles containing or derived from carbohydrates have blossomed over the last decades. Such macrocycles, naturally present in a number of biologically active products from plant and microorganism, have attracted great interest due to their structural complexity and the synthetic challenges associated with their total synthesis. More recently, an increasing number of studies have been devoted to the preparation of structurally simpler unnatural structures for biological, chemical, or analytical applications. Many advantages are associated with carbohydrate-derived structures. First, carbohydrates are readily accessible from natural source; the existence of several stereoisomers allows the design and synthesis of a large variety of macrocycles. Second, the multifunctionality of carbohydrte not only provides the possibility of linkage through the different positions of sugar ring so as to enlarge the structure diversity, but also allows a modulation of the physicochemical properties (like solubility, hydrophilic/lipophilic balance, biodisponibility, etc.). Third, the presence of a furanoid or pyranoid cycle imposes geometric constraints, which is highly desirable for the design of conformationally restricted molecular platforms. Furthermore, the chiral nature of carbohydrates allows the preparation of chiral cavities, which can be useful in the field of asymmetric catalysis and chiral recognition. Finally, synthesis of carbohydrate-derived macrocycles using sugar building o blacks such as sugar amino acids (sugars containing both an amino and a carboxylic acid group) offers the possibility to access a variety of compounds in a modular way.