Abstract

AbstractBiocatalytic carbon‐carbon bond formation by means of aldolases offers an exceptionally stereoselective and green tool for this strategic reaction in synthetic organic chemistry. Recent developments have shown that aldolases are particularly suitable catalysts for asymmetric framework construction and preparation of innovative molecules, which are valuable for investigations in drug discovery. Finding novel carboligases with unprecedented activities and engineering those available for improved substrate tolerance and stereoselectivity towards new synthetic challenges are fostering the advances in this field. Extensive knowledge of the precise reaction mechanism and the enzyme‐substrate interactions arising from biochemical and structural studies are leading to the development of novel catalysts by rational strategies, as well as to de novo computational design of enzymes. Besides, a number of industrially‐oriented processes with aldolases have been developed towards the production of drug precursors and dietary commodities.

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