Automated Enzyme Screening Methods for the Preparation of Enantiopure Pharmaceutical Intermediates

In a pharmaceutical environment, the need for efficient and practical screening techniques has become vital in the search for ideal enzymes that can be used in the preparation of drug intermediates. This paper describes a general high throughput screening (HTS) protocol that has been validated by a number of global projects within Pfizer. It outlines the procedures for the preparation of screening kits, as well as protocols for reaction set‐up, optimization and analysis. The need for such protocols in routinely evaluating the use of solvent engineering in enzymatic hydrolysis reactions is also outlined, with several examples provided. The advantages and disadvantages of a number of complementary analytical tools that are being used in the analysis of enzymatic reactions are also discussed.