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

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• 作者：Elena Fern谩ndez-脕lvaro ; Jorge Esquivias ; Mar铆a P茅rez-S谩nchez ; Pablo Dom铆nguez de Mar铆a ; Modesto J. Remui帽谩n-Blanco
• 关键词：CAL-B ; Enantioselective biotransformations ; Tetrahydropyrazolo[1 ; 5-伪]pyrimidines ; Therapeutic agents
• 刊名：Journal of Molecular Catalysis B: Enzymatic
• 出版年：February, 2014
• 年：2014
• 卷：100
• 期：Complete
• 页码：1-6
• 全文大小：899 K

文摘

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.