Direct alkene functionalization via photocatalytic hydrogen atom transfer from C(sp3)–H compounds: a route to pharmaceutically important molecules

Abstract

Direct functionalization of alkenes with C(sp³)–H substrates offers unique opportunities for the rapid construction of pharmaceuticals and natural products. Although significant progress has been made over the past decades, the development of green, high step-economy methods to achieve these transformations under mild conditions without the need for pre-functionalization of C(sp³)–H bonds remains a substantial challenge. Therefore, the pursuit of such methodologies is highly desirable. Recently, the direct activation of C(sp³)–H bonds via photocatalytic hydrogen atom transfer (HAT), especially from unactivated alkanes, has shown great promise. Given the potential of this approach to generate a wide range of pharmaceutically relevant compounds, this review highlights the recent advancements in the direct functionalization of alkenes through photocatalytic HAT from C(sp³)–H compounds, as well as their applications in the synthesis and diversification of drugs, natural products, and bioactive molecules, aiming to provide medicinal chemists with a practical set of tools.