Tunable microwave-assisted method for the solvent-free and catalyst-free peracetylation of natural products

Manuela Oliverio, Paola Costanzo, Mónica Nardi, Carla Calandruccio, Raffaele Salerno, Antonio Procopio

Beilstein Journal of Organic Chemistry · 2016 · 23 citations · 38 references

DOIFull text

Open access

Abstract

<b>Background:</b> 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. <b>Results:</b> 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. <b>Conclusion:</b> 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.

References

38