Engineering Research Centre of Pharmaceutical Process Chemistry, Ministry of Education, Shanghai Key Laboratory of New Drug Design, School of Pharmacy, East China University of Science and Technology, 130 Meilong Road, 200237, Shanghai, China.
School of Biomedical and Pharmaceutical Sciences, Guangdong University of Technology, 510006, Guangzhou, China.
Chemistry. 2023 May 22;29(29):e202300367. doi: 10.1002/chem.202300367. Epub 2023 Apr 13.
A straightforward synthesis approach to chiral 1-aryl-2-aminoethanols via the one-pot asymmetric hydrogenation catalyzed by Ir catalyst was developed. This tandem process involves the in situ generation of α-amino ketones via the nucleophilic substitution of α-bromoketones with amines and the Ir-catalyzed asymmetric hydrogenation of ketone intermediates to provide diverse enantiomerically enriched β-amino alcohols. The excellent yields and enantioselectivities (up to 96 % yield and up to >99 % ee) with a wide substrate scope in this one-pot strategy were obtained.
发展了一种通过 Ir 催化剂一锅不对称氢化反应直接合成手性 1-芳基-2-氨基乙醇的方法。该串联过程涉及通过亲核取代α-溴代酮与胺生成α-氨基酮，以及 Ir 催化的酮中间体的不对称氢化，从而提供多种对映体富集的β-氨基醇。该一锅法具有广泛的底物范围，获得了优异的产率和对映选择性（高达 96%的产率和高达>99%的对映体过量）。
