The introduction of fluorine atoms as substitutes for hydrogen is an important strategy for the modulation of the biological activity of pharmaceutically relevant molecules. Considerable efforts in the scientific community have therefore been devoted to the development of new synthetic methodologies for accessing fluorinated compounds. In general, approx. 50% of new small molecule pharmaceuticals entering phase clinical studies contain fluorine.

In a paper published in Angewandte Chemie International Edition, DOI: 10.1002/anie.201604152, a team consisting of Thomas L. Andersen, Mette W. Frederiksen, Katrine Domino and Prof. Troels Skrydstrup have devised a novel means of preparing elaborate fluorinated small building blocks, which will be useful for the development of fluorine-containing pharmaceuticals.

Their method relies on a novel palladium-catalysed carbonylation of bromodifluoroacetamides and –acetates, providing good yields of these novel building blocks.