King Abdullah University of Science and Technology (KAUST) KAUST Catalysis Center (KCC) , Thuwal 23955-6900 , Saudi Arabia.
Institute of Organic Chemistry , RWTH Aachen University , Landoltweg 1 , Aachen 52074 , Germany.
J Am Chem Soc. 2019 Dec 11;141(49):19415-19423. doi: 10.1021/jacs.9b10364. Epub 2019 Nov 27.
A series of methyl aluminum complexes bearing chiral biphenol-type ligands were found to be highly active catalysts in the asymmetric reduction of heterocyclic ketones (S/C = 100-500, ee up to 99%). The protocol is suitable for a wide range of substrates and has a high tolerance to functional groups. The formed 2-heterocyclic-alcohols are valuable building blocks in drug discovery or can be used as ligands in asymmetric catalysis. Isolation and comprehensive characterization of the reaction intermediates support a catalysis cycle proposed by DFT calculations.
一系列带有手性联苯型配体的甲基铝配合物被发现是杂环酮不对称还原的高效催化剂（S/C = 100-500，ee 值高达 99%）。该方法适用于广泛的底物，对官能团具有很高的容忍度。形成的 2-杂环醇是药物发现中的有价值的构建块，也可用作不对称催化中的配体。反应中间体的分离和综合表征支持由 DFT 计算提出的催化循环。
