Enzymatic cascades for the regio- and stereoselective synthesis of chiral amines

Significant advancements in protein engineering and DNA technology have seen biocatalytic transformations take the place of traditional chemical manipulations in both academia and industry for the preparation of active pharmaceutical ingredients (APIs) and other medicinally relevant compounds. However, despite the large repertoire of commercially available biocatalysts that are readily accessible, enzymes which mediate the formation of C–C bonds and those that enable convergent synthesis remain largely undeveloped. To expand the scope of biocatalytic retrosynthesis and enable it to complement traditional chemical retrosynthesis it is essential to develop a ‘toolbox’ of biocatalysts which build molecular complexity. Of particular interest is the development of one-pot enzymatic cascades for the synthesis of functionalised, chiral building blocks without the need for protecting group manipulations or harsh reaction conditions. Highly regio- and stereoselective chemoenzymatic cascades have been developed for the synthesis of a range of chiral amines employing ω-transaminases and monoamine oxidase variants.