Research Article  |  Published 23 March 2019

Halogenation – A Versatile Tool For Drug Synthesis - The Importance Of Developing Effective And Eco-Friendly Reaction Protocols 

Alexandra Jităreanu*, Ioana Cezara Caba, Luminita Agoroaei

Toxicology Department, University of Medicine and Pharmacy „Grigore T. Popa” Iaşi, Faculty of Pharmacy, Universitatii street no 16, Iaşi, Romania


The preoccupation for discovering new therapeutic agents is constant and, in this context, the study of bromine-containing molecules is a research field of great interest. These compounds exhibit a wide range of biological activities and bromination can be considered an effective tool to enhance the potency of bioactive agents. Accordingly, it is very important to find new efficient ways for the synthesis of brominated derivatives. This review focuses on presenting several bromination techniques available at present, emphasizing the advantages and disadvantages associated with each reaction protocol, in search for the most effective ways to insert bromine atoms in different molecules, that are both eco-friendly and efficient. Currently, several bromination strategies are presented in literature, but the modern trend is oriented towards new techniques, that do not affect the environment and reduce to the minimum the consumption of harmful reagents and solvents. Traditional synthetic methods also lack specificity and regioselectivity. Biological halogenation can represent the future for obtaining the desired brominated compounds, the use of enzymes for halogenation being potentially the most effective and environmentally friendly route, but the transfer of this technology to industrial large manufacturing scale was not yet made. An improved understanding of biological halogenation and the progress in the field of enzyme engineering could lead to the development of novel synthetic methods for the creation of new compounds, involving stable and selective biocatalysts.

biocatalysts, bromination, eco-friendly, haloperoxidases, liquid bromine, oxidative bromination, quaternary ammonium tribromides.

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