A Personal Account on Industrial Collaborations in the Field of C–H Activation

Abstract

In recent years, transition-metal-catalyzed C–H functionalization has emerged as a potentially greener alternative to classic cross-couplings and as a powerful tool to access complex functional molecules with improved step-economy. This short account relates our experience of industrial collaborations in C(sp³)–H bond activation, which were key to the development of this topic in our group. The synthesis of the antianginal drug Ivabradine led us to develop a general approach to benzocyclobutenes, which were further employed in pericyclic reactions. A follow-up study led us to discover a new method to construct arylcyclopropanes via double C–H activation and the coupling of two alkyl groups. Finally, targeting the herbicide Indaziflam contributed to develop C(sp³)–H activation as a powerful tool to access a variety of relevant indane motifs. We hope that these successful stories will help to stimulate further fruitful Industry-Academia collaborations in the field of synthetic chemistry.