Assessing biocatalysis for the synthesis of optically active tetrahydropyrazolo[1,5-α]pyrimidines (THPPs) as novel therapeutic agents.

Highlights: [•] Enzymatic screening to identify the potential application of biocatalysis to therapeutically relevant substrates: tetrahydropyrazolo[1,5-α]pyrimidines. [•] CAL-B-catalyzed enantioselective biotransformations: kinetic resolution of chiral substrates with asymmetric centres located far from the catalytic centre. [•] Proof of concept for process optimization: screening of bio-based co-solvents. [ABSTRACT FROM AUTHOR]