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Carbohydrates, being the most abundant class of biopolymers on earth, have, due to their structural diversity and inherent chirality, been subject to comprehensive biological investigations. Their biological importance is unquestionable, as a wide range of biological recognition and communication phenomena depend on complex oligo- and polysaccharide structures. This also makes carbohydrates attractive targets for developing new pharmaceuticals. In this chapter, a fundamental overview of the synthesis of oligosaccharides from the viewpoint of both traditional synthetic methods as well as fully automated methodologies is provided. Furthermore, selected commercially available oligosaccharide pharmaceuticals as well as promising new compounds under development are briefly discussed.

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