Department of Chemistry , University of Illinois at Urbana-Champaign , 600 S. Mathews , Urbana , Illinois 61801 , United States.
Department of Process Research and Development , Merck & Co., Inc. , Rahway , New Jersey 07065 , United States.
J Am Chem Soc. 2019 Jan 16;141(2):739-742. doi: 10.1021/jacs.8b09811. Epub 2019 Jan 7.
A Rh-catalyzed enantioselective hydroamination of allylamines using a chiral BIPHEP-type ligand is reported. Enantioenriched 1,2-diamines are formed in good yields and with excellent enantioselectivities. A diverse array of nucleophiles and amine directing groups are demonstrated, including deprotectable motifs. Finally, the methodology was demonstrated toward the rapid synthesis of 2-methyl-moclobemide.
报道了一种 Rh 催化的手性 BIPHEP 型配体的烯丙胺的对映选择性氢胺化反应。手性 1,2-二胺以良好的收率和优异的对映选择性得到。展示了各种亲核试剂和胺导向基团，包括可脱保护的基序。最后，该方法被用于快速合成 2-甲基-吗氯贝胺。
