Glycoproteins and glycolipids play central roles in human health and disease, and their mimetics are primary candidates for drug development. Our understanding of the molecular level of phenomena based on molecular recognition of oligosaccharides by specific receptors has taken tremendous advantage from their chemical synthesis, which provides homogeneous material not attainable from biosynthetic systems. This review summarizes chemoselective approaches for the assembly of neoglycoconjugates. The objective of these methods is to make glycoconjugate synthesis accessible to a broader community, thus accelerating progress in biotechnology.