As medicinal chemistry finds the need to access more stereochemically diverse molecular structures, it is unsurprising that there is an increasing desire for chemical transformations that are more cost-effective, atom economical, robust, and translatable from the small reaction vessel to the pilot plant reactor.  Biocatalysis often meets these requirements for a growing number of reactions when compared to its transition metal catalyst counterparts, and has been increasingly adopted as a preferred option in late stage route development and manufacture. Technological improvements in directed evolution, molecular biology, gene sequencing, and automation have resulted in a continually improving biocatalytic toolbox of chemical transformations.  Despite the surge of activity in this field over the past decade, the adoption of enzymatic catalysis earlier in the discovery process by medicinal chemists has paled in comparison to its use in late stage processes.  This talk will address some of the technical and philosophical challenges to adoption and also highlight examples from our discovery chemistry efforts at GSK

Biocatalysis in medicinal chemistry – a perspective

ACS Spring 2022

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