«Evolved Aliphatic Halogenases Enable Regiocomplementary C‐H Functionalization of an Added‐Value Chemical» by Takahiro Hayashi, Mathieu Ligibel, Emine Sager, Moritz Voss, Jürg Hunziker, Kirsten Schroer, Radka Snajdrova and Rebecca Buller

Non‐heme iron halogenases are synthetically valuable biocatalysts with exquisite stereo‐ and regioselectivity. However, the reported substrate scope is limited. Using structure‐guided evolution we engineered the recently discovered halogenase WelO5* for chlorination of a pharmaceutical interesting martineline-derived fragment and identified key positions in the active site.

Our report provides the first example of expanding the substrate scope of this type of halogenases beyond the native substrates and underscores the usefulness of this family of enzymes for late stage halogenation of value-added chemicals.

Angew. Chem. Int. Ed. 10.1002/anie.20190724