Highly Stereoselective Biocatalytic Reductions for the Synthesis of Chiral Intermediates(Abstracts)

摘要

The asymmetric reduction of ketones is one of the most important, fundamental and practical reactions for producing non-racemic chiral alcohols, which can be transformed into various functionalities, without racemization, to synthesize industrially important chemicals such as pharmaceuticals, agrochemicals and natural products. Biocatalytic reduction of α-alkyl-1,3-diketones 1, and α-alkyl-β-keto esters employing isolated NADPH-dependent ketoreductases (KREDs) proved to be a highly efficient method for the preparation of optically pure keto-alcohols 2, 1,3-diols 3 or hydroxy esters.[3,4] These chiral compounds are very important in asymmetric organic synthesis, where they are used as building blocks for synthesis of polyketides, statins, protease inhibitors, and other important pharmaceuticals. The ability to synthesize various single diastereomers of the same compound, is desirable when libraries of pharmaceutical compounds are synthesized and tested for biological activity.