For the planningo fa no rganic synthesis route, the disconnection approach guided by retrosynthetic analysis of possible intermediates and the chemical reactions involved, backt or eady available starting materials, is well established. In contrast, such concepts just get developed for biocatalytic routes. In this Review we highlightf unctional group interconversions catalyzed by enzymes. The article is organized rather by chemical bonds formed-exemplified for CÀN, CÀO-and CÀC-bonds-and not by enzyme classes, covering ab road range of reactions to incorporate the desired functionality in the target molecule. Furthermore, the successful use of biocatalysts, also in combination with chemicals teps, is exemplified for the synthesis of various drugs and advanced pharmaceutical intermediates such as Crispine A, Sitagliptina nd Atorvastatin. This Reviewa lso provides some basic guidelines to choose the most appropriate enzyme for at argeted reaction keepingi nm ind aspects like commercial availability,c ofactor-requirement, solventt olerance, use of isolated enzymes or whole cell recombinant microorganisms aiming to assist organic chemists in the use of enzymesf or synthetic applications.