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Updated: Jan 16, 2026

Synthesis of a Borylated Ibuprofen Derivative Through Suzuki Cross-Coupling and Alkene Boracarboxylation Reactions
Published on: November 30, 2022
C(sp2)-C(sp3) Suzuki-Miyaura Cross-Coupling Using gem-Bis(boronates)
Jun Xiao1, Wen Xiu2, Qingjian Zhang3
1Pfizer Research and Development, 280 Shennecossett Road, Groton, Connecticut 06340, United States.
Abstract:
A strategy utilizing gem-bis(boronates) as a stable and easily accessible surrogate for the analogous monoboronate and their efficient use in Suzuki-Miyaura cross-couplings to access the highly interesting 1,2-diaryl ethane motif is described. The general reactivity of gem-bis(boronates) and its advantages over monoboronate are demonstrated by a broad substrate scope and minimal β-hydride elimination side product formation. Cusparine, an antituberculosis natural product, was synthesized via this method with a shortened route, demonstrating its brevity, effectiveness, and scalability.
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