The worldwide yearly sales are about 4.6 billion US$ and the patent is going to expire in December 2018. The synthesis has already been optimized by using enzymatic steps instead of “old-fashioned” chemistry according to Pfizer´s green chemistry policy.

Our aim is to reduce the use of solvents and catalysts to save the environment and also to use the new enzymatic step as platform technology for other synthesis. Another aspect in this new root is an enantiomeric selectivity which results in a higher yield and less waste. The desired enzymatic step in our synthesis is a reductive amination.

The chemical way for a reductive amination uses a metal catalyst (here it´s nickel) and is rarely selective relating to the enatiometry. By using Alanine as strong amine donor and a Transaminase, it is highly possible to gain a much better selectivity of the desired product under “normal” conditions.

First we will screen our enzymatic database on this ambitious reaction with a chirality center in ß-position and if needed, trials are going to be performed to optimize the activity and selectivity. In the end the reaction will be tested according to an ecological efficiency and cost-effectiveness. The long term goal should be to establish this step as an enzymatic cascade in a microorganism.

Project Operation:

Universität Greifswald
Institut für Biochemie
Jun. Prof. Dr. Matthias Höhne
Felix-Hausdorff-Str. 4
17487 Greifswald

Herbrand PharmaChemicals GmbH
Dr. Martin Erhardt
Brambachstr. 31
77723 Gengenbach

Universität Rostock
Institut für Chemie
Prof. Dr. Udo Kragl
Albert-Einstein-Str. 3a
18059 Rostock

Enzymicals AG
Dr. Ulf Menyes
Walther-Rathenau-Str. 49a
17489 Greifswald

Ref. 31842