In order to meet the increasing demands for the development of large varieties of new molecules for discovering new drugs and materials, organic chemists are developing many novel multifunctional building blocks, which are assembled rationally to create ‘nature-like’ and yet unnatural organic molecules with well-defined structures and useful properties. Sugar amino acids(SAAs), the carbohydrate derivatives bearing both amino and carboxylic acid functional groups, are important ones of these multifunctional building blocks, which can be used to create novel materials with potential applications as glycomimetics and peptidomimetics. This review will focus on recent synthetic strategies of SAAs and their applications in creating large number of structurally diverse glycomimetics and peptidomimetics. In order to meet the increasing demands for the development of large varieties of new molecules for discovering new drugs and materials, organic chemists are developing many novel multifunctional building blocks, which are assembled rationally to create ’nature-like’ and yet unnatural organic molecules with well-defined structures and useful properties. Sugar amino acids (SAAs), the carbohydrate derivatives bearing both amino and carboxylic acid functional groups, are important ones of these multifunctional building blocks, which can be used to create novel materials with potential applications as glycomimetics and peptidomimetics. This review will focus on recent synthetic strategies of SAAs and their applications in creating large number of structurally diverse glycomimetics and peptidomimetics.