Dr. Heng-Hui Li, Yuwen Liu, Prof. Dr. Søren Kramer
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Benzylic C(sp3)−H Phosphonylation via Dual Photo and Copper Catalysis
Alkyl phosphonates are important motifs in medicinal chemistry, yet their efficient synthesis by direct C(sp3)−H functionalization remains a challenge. Here, we report straightforward access to benzylic phosphonates by direct C(sp3)−H functionalization in a cross-dehydrogenative-coupling reaction between non-specialized alkylarenes and unfunctionalized phosphites. Notably, the C−H substrates are used as the limiting reagents. The scope of benzylic C−H substrates is broad, and the mild reaction conditions allow for good functional group tolerance. Mechanistic studies indicate that the reaction proceeds via a radical pathway rather than the cationic pathway followed for specialized benzylic C−H substrates in previous methods.
期刊介绍:
Angewandte Chemie, a journal of the German Chemical Society (GDCh), maintains a leading position among scholarly journals in general chemistry with an impressive Impact Factor of 16.6 (2022 Journal Citation Reports, Clarivate, 2023). Published weekly in a reader-friendly format, it features new articles almost every day. Established in 1887, Angewandte Chemie is a prominent chemistry journal, offering a dynamic blend of Review-type articles, Highlights, Communications, and Research Articles on a weekly basis, making it unique in the field.