Solvent-free, Catalyst-free Peracetylation of Natural Products

Background: 

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.

Results:

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. 

Conclusion: 

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.

Reference:

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