Biocatalysis was an important technology for the synthesis of a gamma secretase modulator. Chemoenzymatic approaches involving transaminases or ketoreductases were evaluated during route scouting. A route using a ketoreductase was selected for further development resulting in an efficient, scalable, second generation process. The ketoreductase was improved by enzyme engineering to enable a multi-kg scale up.

Development of a chemoenzymatic process for a gamma secretase modulator

256th National Meeting (2018)

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