The use of biocatalyzed processes is increasingly becoming recognized as a very important part inside Green Chemistry, because those synthetic routes mediated by enzymes or cells are generally conducted under mild reaction conditions, at ambient temperature and can use water as reaction medium in many cases. Their high selectivity avoids the need of functional group activation and protection/deprotection steps usually required in traditional organic synthesis. Thus, biocatalysis provides processes which are shorter, produce less waste and reduce manufacturing costs and environmental impact. These features are even more significant in drug synthesis, because it is well known that Pharma Industry is the most waste-producers. In this review some biocatalyzed protocols for the preparation of bioactive molecule and/or chiral building blocks for drug synthesis will be presented, focusing only in those used for treatment of noncommunicable diseases (NCDs).