The peracetylation is a simple chemical modification that can be used to enhance the bioavailability of hydrophilic products and to obtain safe and stable pro-drugs.
A totally green, solvent-free and catalyst-free microwave (MW)-assisted method for peracetylation of natural products such as oleuropein, alpha-hederin, quercetin and rutin is presented. By simply tuning the MW heating program, polyols with chemical diverse -OH groups or thermolabile functionalities can be peracetylated to improve the biological activity without degradation of the natural starting molecules. An evaluation of the process greenness was performed.
The method is potentially universally applicable for green acetylation of hydrophilic biological molecules, potentially easily scalable for industrial applications, including pharmaceutical, cosmetic and food industry.
Oliverio, M., Costanzo, P., Nardi, M., Calandruccio, C., Salerno, R., & Procopio, A. (2016). Tunable microwave-assisted method for the solvent-free and catalyst-free peracetylation of natural products. Beilstein Journal of Organic Chemistry, 12, 2222-2233. doi:10.3762/bjoc.12.214