Direct Borylation of Primary CH Bonds in Functionalized Molecules by Palladium Catalysis |
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| Authors: | Li‐Sheng Zhang Guihua Chen Xin Wang Qing‐Yun Guo Xi‐Sha Zhang Fei Pan Kang Chen Prof Dr Zhang‐Jie Shi |
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| Institution: | 1. Beijing National Laboratory of Molecule Science (BNLMS) and Key Laboratory of Bioorganic Chemistry and Molecular Engineering of the Ministry of Education, College of Chemistry and Green Chemistry Center, Peking University, Beijing, 100871 (China);2. State Key Laboratory of Organometallic Chemistry, Chinese Academy of Science, Shanghai, 200032 (China) |
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| Abstract: | Organoborane compounds are among the most commonly employed intermediates in organic synthesis and serve as crucial precursors to alcohols, amines, and various functionalized molecules. A simple palladium‐based system catalyzes the conversion of primary C(sp3)? H bonds in functionalized complex organic molecules into alkyl boronate esters. Amino acids, amino alcohols, alkyl amines, and a series of bioactive molecules can be functionalized with the use of readily available and removable directing groups in the presence of commercially available additives, simple ligands, and oxygen (O2) as the terminal oxidant. This approach represents an economic and environmentally friendly method that could find broad applications. |
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| Keywords: | amino acids borylation C H functionalization directing groups palladium |
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