Organic O-sulfates and N-sulfamates have a number of crucial biological applications, ranging from the metabolism of xenobiotics to the downstream signalling of steroidal sulfates in pathological conditions. Anti-coagulant, anti-viral, anti-inflammatory, immunomodulatory, and anti-tumour properties have been associated with sulfated polysaccharides, flavonoids, steroids, and proteins. Heparin and heparan sulfate are examples of glycosaminoglycans (GAGs) that contain sulfate groups which promote molecular interactions with protein ligands and binding at the cellular surface. The incorporation of polar, hydrophilic sulfate groups onto drug-like molecules has facilitated the investigation of novel sulfated biomolecules as potential new therapies. However, the chemical synthesis and purification of sulfated compounds are challenging when one or more sulfate groups are present, due to both anionic crowding, lack of regioselectivity, and poor solubility in organic solvents. [20] Successfully sulfated compounds remain sensitive to both acidic and high temperature reaction environments. . As a result, the sulfation reaction is often the last step in a synthetic process, which restricts any potential chemical modifications. Given the growing interest in sulfation and the significant biological functions of sulfated molecules, several synthetic approaches to sulfate oxygen, nitrogen, oxime, and phosphate functionalities have been developed. This essay will explore the most commonly encountered and latest chemical sulfation approaches that have been applied to a wide range of small and biomolecules since the last major review in 2010. Sulfation using sulfuric acid and related reagents.