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Updated: May 3, 2026
Synthesis of a Borylated Ibuprofen Derivative Through Suzuki Cross-Coupling and Alkene Boracarboxylation Reactions
Published on: November 30, 2022
Precise borylation of targeted methyl group via an orderly chain-walking strategy
Yinwei Bao1, Chenke Hu1, Lixuan Zheng1
1Center of Chemistry for Frontier Technologies, State Key Laboratory of Soil Pollution Control and Safety, Department of Chemistry, Zhejiang University, Hangzhou 310058, China.
None:
C─H functionalization is an attractive approach in organic synthesis due to its directness and efficiency. Nevertheless, achieving precise differentiation among multiple methyl groups with highly similar chemical environments remains a notable challenge. Here, an orderly chain-walking borylation strategy was introduced via targeted hook and enduring slide that enables precise remote C(sp3)-H borylation and affords a series of "Y-shape" boron analogs through rational desymmetric ligand design. This method exhibits broad substrate scope, good functional group tolerance, and high atom economy and achieves a chain-walking distance of 32 carbons, and we hope it will promote cross-disciplinary innovation in areas including materials science and pharmaceuticals.
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