Sulfation is one of the most important modifications that occur to a wide range of small biomolecules including polysaccharides, proteins, flavonoids, and steroids. Historically, the incorporation of sulfate moiety to an appropriate substrate, results in an increase of the substrate's hydrophilicity and therefore facilitate its elimination from the body. However, sulfated scaffolds such as polysaccharides, proteins, flavonoids, and steroids have significant biological and pharmacological roles such as cell signalling, modulation of immune and inflammation response, anticoagulation, antiatherosclerosis, and antiadhesive. It is imperative that sulfated molecules can be easily prepared for furthering the biological understanding of the role of sulfate in the body.