Tailor-made enzymes with modiﬁed activity and the preparation of thermostable and pH stable enzymes produced by random and site-directed mutagenesis have lead to the production of novel stereoselective biocatalysts. The use of enzymes in organic solvents has led to hundreds of publications on enzyme-catalyzed asymmetric synthesis and resolution processes. Molecular recognition and selective catalysis are key chemical processes in life which are embodied in enzymes. A number of review articles have been published on the use of biocatalysis in organic synthesis. This chapter provides different approaches towards the use of microbial enzymes for the synthesis of chiral intermediates for Omapatrilat 1 by three different routes. Omapatrilat 1 is an antihypertensive drug which acts by inhibiting angiotensin-converting enzyme (ACE) and neutral endopeptidase.