Direct alkene functionalization via photocatalytic hydrogen atom transfer from C(sp3)-H compounds: a route to
Hangqian Fan1, Yuxin Fang1, Jingbo Yu1
1Laboratory of Pharmaceutical Engineering of Zhejiang Province, Key Laboratory for Green Pharmaceutical Technologies and Related Equipment of Ministry of Education, Collaborative Innovation Center of Yangtze River Delta Region Green Pharmaceuticals, Zhejiang University of Technology, Hangzhou 310014, P. R. China. yjb@zjut.edu.cn.
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.
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