The production of ever more complex fine chemicals for life sciences (health care, agrochemicals, nutraceuticals) requires selective synthetic biotechnological tools, which complement purely organic chemical synthesis with a rewarding economic and ecological impact. Biotechnology has become an important contributor to the gross domestic product in many countries, and this contribution translates also into enzyme applications for different markets and products, novel biotech companies, and international research programs and consortia. The present chapter deals with the different aspects of enzyme biocatalysis for chemical transformations, starting with the prospection and identification of novel microbial enzymes, which are becoming indispensable for current industrial processes. The benefits of extremophilic bioprospection and protein engineering along with the preponderant role of nature itself as the best source for finding truly novel enzymes with potential industrial applicability are discussed. Also, the different production processes, using immobilized and free biocatalysts for fine and bulk chemical production, are analyzed. Finally, new reactions and developments in enzymatic catalysis will be presented as well as green chemistry aspects as an inherent feature of industrial biotransformation, where novel technologies for cofactor regeneration and solvents for biotransformations are featured as “green” solutions.