Robust Enzymatic Resolution of 3-Fluoromandelic Acid with Lipase PS Supported on Celite

The resolution of different mandelic acids using the lipase PS “Amano” SD enzyme is described. By supporting the lyophilized enzyme over Celite, both the activity and the stability of lipase PS in organic media were significantly improved, enabling the robust resolution scale-up of 3-fluoromandelic acid. The methodology was extended to produce a range of optically pure (<i>R</i>)-mandelic acids, avoiding tedious extractions or chromatography

Transaminases Applied to the Synthesis of High Added-Value Enantiopure Amines

Critical parameters affecting the stereoselective amination of (hetero)­aromatic ketones using transaminases have been studied, such as temperature, pH, substrate concentration, cosolvent, and source and percentage of amino donor, to further optimize the production of enantiopure amines using both (<i>S</i>)- and (<i>R</i>)-selective biocatalysts from commercial suppliers. Interesting enantiopure amino building blocks have been obtained, overcoming some limitations of traditional chemical synthetic methods. Representative processes were scaled up, affording halogenated and heteroaromatic amines in enantiomerically pure form and good isolated yields