Department of Chemistry, School of Science, The University of Tokyo, 7-3-1, Hongo, Bunkyo-ku, Tokyo 113-0033, Japan.
J Am Chem Soc. 2020 Sep 30;142(39):16546-16551. doi: 10.1021/jacs.0c08109. Epub 2020 Sep 14.
Heterogeneous chiral Rh catalysts based on acid-base and electrostatic interactions have been developed. The robust catalysts demonstrate high activity and selectivity in the continuous-flow asymmetric hydrogenation of a wide variety of enamides and dehydroamino acids, providing optically active amides without leaching of metal species. The chiral environments can be easily tuned by changing the chiral ligands, demonstrating the high versatility of the heterogeneous catalysts. By applying these efficient catalysts, continuous synthesis of several active pharmaceutical ingredient intermediates was achieved.
基于酸碱和静电相互作用的非均相手性 Rh 催化剂已被开发出来。这些坚固的催化剂在各种烯酰胺和脱氢氨基酸的连续流不对称氢化反应中表现出高活性和选择性,提供了手性酰胺,而金属物种没有浸出。通过改变手性配体,可以很容易地调整手性环境,显示出非均相催化剂的高多功能性。通过应用这些高效催化剂,实现了几种活性药物成分中间体的连续合成。