Biocatalysis offers mild reaction conditions, an environmentally attractive catalyst–solvent system, high activities, and chemo-, regio-, and stereoselectivities, while the use of enzymes generally circumvents the need for functional group activation and avoids protection/deprotection steps required in traditional organic syntheses. This review, using ß-lactam antibiotics as an example, discusses recent advances in biocatalysis research towards the goal of ‘green’ methodologies for the manufacture of (fine) chemicals and the emulation of a cell's enzymatic cascade processes.