Abstract
Fluoroalkylations have received increasing attention in the academic and industrial environment due to the particular properties of the active ingredients that are strongly influenced by fluoroalkyl substituents. The inherent difficulties of introducing a fluoroalkyl substituent into advanced intermediates has triggered the development of an enormous number of specialized reagents, which, however, are often not suitable for large scale applications. In contrast to this reagent based fluoroalkylation approach, the direct activation of industrially readily available fluoroalkyl halides could be more suitable for a large-scale process. In this way the dithionite initiated fluoroalkylation as well as newly developed catalytically activated fluoroalkylation protocols were considered for industrial large-scale applications.
Highlights
Numerous active ingredients in the pharmaceutical and agrochemical industries as well as material sciences[1] contain fluorine as a crucial part, determining the desired properties of the ingredient to a large extent
Nearly 60% of the active ingredients for the agrochemical industry contain fluorine. Most of these products contain fluorine in form of a fluoroalkyl group. The introduction of such fluoroalkyl groups has been subject to an enormous amount of academic activity with an ever-increasing number of publications appearing in all major chemistry journals (Science Finder, Fig. 1)
Focusing on large-scale production of fluoroalkylated products, we identified the need for industrially viable fluoroalkylation methods that allow the introduction of fluoroalkylation substituents at a late stage, making use of industrially available starting materials and avoiding the use of expensive and waste intensive reagents
Summary
Numerous active ingredients in the pharmaceutical and agrochemical industries as well as material sciences[1] contain fluorine as a crucial part, determining the desired properties of the ingredient to a large extent. The currently available industrial products containing fluoroalkyl groups are almost exclusively produced by a so-called ‘downstream’ approach This approach makes use of fluorinated starting materials with the desired fluorine substituents in place at a very early stage. The development of a fluoroalkylation reaction for an industrial large-scale process requires the consideration of numerous aspects such as toxicity-, waste- and environmental-, corrosion-, and energetic- (thermodynamics and kinetics) issues and the cost arising from the selection of starting materials. With these requirements in mind, we focused on two general methods for the industrial fluoroalkylation: 1.
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