Enzyme catalysis is gaining increasing importance in synthetic chemistry. Nowadays, the growing number of biocatalysts accessible by means of bioinformatics and enzyme engineering opens up an immense variety of selective reactions. Biocatalysis especially provides excellent opportunities for late‐stage modification often superior to conventional de novo synthesis. Enzymes have proven to be useful for direct introduction of functional groups into complex scaffolds, as well as for rapid diversification of compound libraries. Particularly important and highly topical are enzyme‐catalysed oxyfunctionalisations, halogenations, methylations, reductions, and amide bond formations due to the high prevalence of these motifs in pharmaceuticals. This Review gives an overview of the strengths and limitations of enzymatic late‐stage modifications using native and engineered enzymes in synthesis while focusing on important examples in drug development.

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Biocatalytic late‐stage modifications offer attractive methods to selectively functionalise complex molecules. Amidst an ever‐growing number of enzymes, modular toolboxes of enzymatic transformations have been made available in synthesis today. Vast sets of biocatalysts are able to address manifold diversifications of interest, e.g., applied for drug development. In their Review on page 16824, Nicholas J. Turner, Christian Schnepel et al. discuss the present array of enzymatic late‐stage modification.

Biokatalytische Modifikationen bieten attraktive Methoden für die selektive Funktionalisierung von komplexen Molekülen. Inmitten einer ständig wachsenden Zahl von Enzymen sind heute modulare Werkzeugkästen enzymatischer Transformationen in der Synthese verfügbar. Eine große Zahl von Biokatalysatoren ist in der Lage, vielzählige Diversifikationen vorzunehmen, z. B. für die Wirkstoffentwicklung. In ihrem Aufsatz auf S. 16962 stellen Nicholas J. Turner, Christian Schnepel et al. die derzeitige Bandbreite enzymatischer Modifikationen vor.