Roger Adams Laboratory, Department of Chemistry, University of Illinois , Urbana, Illinois 61801, United States.
J Am Chem Soc. 2017 Mar 15;139(10):3805-3821. doi: 10.1021/jacs.6b13384. Epub 2017 Mar 7.
The existence of the oft-invoked intermediates containing the crucial Pd-O-B subunit, the "missing link", has been established in the Suzuki-Miyaura cross-coupling reaction. The use of low-temperature, rapid injection NMR spectroscopy (RI-NMR), kinetic studies, and computational analysis has enabled the generation, observation, and characterization of these highly elusive species. The ability to confirm the intermediacy of Pd-O-B-containing species provided the opportunity to clarify mechanistic aspects of the transfer of the organic moiety from boron to palladium in the key transmetalation step. Specifically, these studies establish the identity of two different intermediates containing Pd-O-B linkages, a tri-coordinate (6-B-3) boronic acid complex and a tetra-coordinate (8-B-4) boronate complex, both of which undergo transmetalation leading to the cross-coupling product. Two distinct mechanistic pathways have been elucidated for stoichiometric reactions of these complexes: (1) transmetalation via an unactivated 6-B-3 intermediate that dominates in the presence of an excess of ligand, and (2) transmetalation via an activated 8-B-4 intermediate that takes place with a deficiency of ligand.
在铃木-宫浦偶联反应中,已经证实了含有关键 Pd-O-B 亚基的中间产物(即“缺失的环节”)的存在。低温、快速注射 NMR 光谱学(RI-NMR)、动力学研究和计算分析的应用,使得这些高度难以捉摸的物种的生成、观察和特性得以实现。确认含有 Pd-O-B 物种的中间产物的能力为澄清关键的转移步骤中硼到钯的有机部分转移的机理方面提供了机会。具体而言,这些研究确定了两种不同的含有 Pd-O-B 键的中间体,即三配位(6-B-3)硼酸配合物和四配位(8-B-4)硼酸盐配合物,它们都经历了转金属化反应,导致交叉偶联产物的形成。已经阐明了这些配合物的化学计量反应的两种不同的机理途径:(1)通过在过量配体存在下占主导地位的未活化的 6-B-3 中间体进行转金属化,和(2)通过配体不足时发生的活化的 8-B-4 中间体进行转金属化。