The path to new chemical entities often shows the limitations of existing tools both in biocatalysis and organic chemistry. Organic synthetic procedures to prepare a compound in a target-oriented synthesis can damage other functional parts of the molecule. Protection-deprotection schemes can lead to a dead end, when a certain protecting group cannot be cleaved off. In biocatalysis, on the other hand, the required biocatalytic toolbox and methodology might not be readily available, therefore limiting a biocatalytic approach. New toolboxes, ingredients, and methodologies at the interface of classical organic synthesis and biocatalytic reactions bridge the gap between these two areas. Since product isolation and purification involves a substantial amount of time in the preparation of chemicals, methodologies to simplify these tasks are necessary to get the pure product into the bottle with less work-up time. Efficient and safe new pharmaceuticals, intermediates and analytical reagents need to be prepared under certain safety, health, environmental and economical boundary conditions. Biocatalytic reactions have been shown to overcome these limitations successfully and are becoming increasingly important in industrial manufacturing. Building bridges between biocatalysis and organic synthesis will therefore create roads to new synthetic strategies and technological frontiers of both fundamental and practical interest. (c) 2007 Society of Chemical Industry.