Progress on Selective Acylation of Carbohydrate Hydroxyl Groups

Sugars have always been an important component of drugs, and their design, discovery, synthesis and preparation play an important role in the diagnosis, prevention and treatment of diseases. To synthesize functional oligosaccharides, we need to perform a variety of selective hydroxyl protections of monosaccharides to synthesize functional sugar building blocks. Among these protection reactions, acylation is the most commonly used method to protect the hydroxyl groups in sugars. Regioselective acylation of saccharide hydroxyl groups needs to be achieved by catalysts. How to efficiently synthesize the target products and how to develop more selective, wider ranging, and more environmentally friendly chemical methods are a consistent goal pursued by chemistry researchers. This paper mainly introduces the research progress on six kinds of approaches for the regioselective acylation of sugar hydroxyl groups: those based on organotin, organoboron, organosilicon, metal salts, hydrogen‐bonding small organic molecules and enzyme reagents. Finally, the Minireview also summarizes the advantages and disadvantages of these catalysts and prospects for the selective acylation of sugar hydroxyl groups.