Sulfones: A New Functional Group for Modular Radical Cross-Coupling

Abstract

<div>Cross-coupling chemistry comprises the vast majority of reactions employed in the synthesis of medicines, agrochemicals, and other functional materials. The interest in single-electron-induced coupling chemistry stems from the unique ability of these methods to facilitate the formation of challenging C(sp2)–C(sp3) linkages. This work introduces a new functional group, PT sulfones, for radical cross-coupling, enabling the simplified modular assembly of complex structures in an ordered, practical fashion. The scope of this method is extensively explored, and its strategic application is exemplified through the streamlined preparation of medicinally-oriented fluorine-containing scaffolds that previously required multiple steps, toxic reagents, and non-modular retrosynthetic blueprints. This work has also resulted in the development of five reagents for the rapid assembly of a vast set of structures, many of which contain challenging fluorination patterns. <br></div><div><br></div>

The rise of preprints in chemistry

“…The counter-argument to this is to highlight examples of published research papers that were first shared as preprints. There are many examples, but to select just a few, you can look to the 16-step synthesis of isoryanodane diterpene (+)-perseanol by Han and co-workers 15,16 , the CryoEM methodological paper by Jones and colleagues 17,18 , or the study of modular radical cross-coupling with sulfones by the Baran group and collaborators 19,20 .…”