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

Enantiomerically pure THPPs are useful pharmacological agents in relevant therapeutic areas such as tuberculosis, osteoporosis and hepatitis C. Typically resolved by preparative chiral HPLC, in this work the catalytic approach – via hydrolase-catalyzed kinetic resolution – has been demonstrated for the first time. After biocatalytic successful proof-of-concept, future opportunities for protein engineering and process set-up appear.