Successful application of enzyme cascades in API synthesis

Published: 18-Sep-2015

Rainer Wardenga and Torsten Sehl illustrate how amine-transaminases can be used in a novel two-step biocatalytic route for production of all four stereoisomers of nor(pseudo)ephedrine from inexpensive, achiral starting materials

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The industrial implementation of biocatalysis for the production of pharmaceuticals and fine chemicals has grown substantially over recent years. An upcoming application is the chiral synthesis of optically pure amines using enzymes from the class of transaminases. The process option has been known for many years but it is now seeing renewed and wider interest in the industry because chiral amines are important building blocks and currently the market for active pharmaceutical ingredients (APIs) and agrochemicals accessible with this technology is very large.

It is estimated that today 75% of all pharmaceuticals contain a chiral amine component in their structure

It is estimated that today 75% of all pharmaceuticals contain a chiral amine component in their structure.1 Moreover, it is expected that the importance of the (R)-enantiomers will increase as they have been difficult to access until now with existing technologies. Furthermore, the targeted production of (R)-enantiomers with a transamination process is ecologically and economically more friendly because the asymmetric transamination will lead to a theoretically possible yield of 100%.

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