Abstract

AbstractAs a simple and efficient system, Cu(OAc)2 ⋅ H2O and K2S2O8 can activate H‐phosphonates to produce the corresponding dialkyl phosphoryl radicals. The obtained dialkyl phosphoryl radicals react smoothly with 2‐amino‐1,4‐naphthoquinones, affording accurate preparation of various phosphoryl‐functionalized 2‐amino‐1,4‐naphthoquinones. The developed copper‐catalyzed cross‐dehydrogenative phosphorylation features broad substrate scope, easily available reagents, high atom economy and operational simplicity, which enables a practical avenue for C−P bond formation.

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