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

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. [ABSTRACT FROM AUTHOR]