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 peri cyclic 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.

Keywords

• bioactive molecules
• catalysis
• c-h activation
• palladium