Green Enzymatic Strategies for the Preparation of Chemically and Pharmaceutically Important Enantiomeric Compounds

Dear Colleagues,

There is a continually growing demand for enantiomerically pure products. Enantiomers of chemically and pharmaceutically interesting compounds and their key intermediates or building blocks for their synthesis can be obtained either from transformations of enantiomerically pure compounds called “chiral pool”, involving mostly natural compounds, such as amino acids, carbohydrates, terpenes and steroids, or from asymmetric syntheses (which often involve the use of expensive enantiomerically pure auxiliary reagents). The enzymatic methods for asymmetric synthesis exploiting the biocatalysts’ inherent enantiomer or enantiotope selectivity represent clear advantages. Enzyme-based catalysis is starting to challenge traditional synthetic methods of producing optically active compounds.

By using enzymes in reactions, the previous reactions under harsh conditions can be coaxed to proceed faster under mild conditions (lower temperatures and pressures; neutral pH), with fewer work-up steps and a higher yield, all of which results in the improvement in the reaction’s efficiency and saves energy.

In the last two decades, many efficient enzymatic strategies (kinetic, dynamic kinetic, sequential kinetic resolution of racemates; desymmetrization of meso and prochiral substrates) and new techniques have been published for the synthesis of enantiopure products. Although a great number of innovative enzymatic routes that involve either using a nature-friendly solvent (water, green organic solvent, or supercritical solvent) or refrain from using any added solvent, based on the principle the best solvent is no solvent, have been published. Sustainable mechanoenzymatic kinetic resolution of several racemic compounds, with the use of ball milling, has also been described.

To attain sustainable enzymatic green strategies that allow the large-scale production of high-value enantiomeric pharmaceuticals, agrochemicals and flavor compounds, one must identify the most suitable biocatalyst (a biocatalyst that can be produced from readily available resources and is biodegradable, nonhazardous and nontoxic) and the best nature-friendly reaction conditions. In the frame of design approaches, the physicochemical (e.g. immobilization of the enzyme) and reaction engineering methods (e.g. the use of different acyl donors or nucleophiles, solvents, etc.) will remain important in future developments. Biocatalyst, reactor engineering and investigation of the cascade systems are to be highlighted.

In the present Special Issue, innovative and sustainable green enzymatic strategies for the preparation of chemically or/and pharmaceutically important enantiopure compounds will be analyzed.

Prof. Dr. Enikő Forró
Prof. Dr. László Poppe
Prof. Dr. István Szatmári
Guest Editors

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• green biocatalyst
• sustainable enzymatic strategy
• valuable enantiopure compound
• environmentally-friendly conditions
• biodegradable and non-toxic solvent
• solvent-free system
• supercritical fluid
• green work-up
• green analytical technique