Zhou Zhe, Ma Zhiwei, Behnke Nicole Erin, Gao Hongyin, Kürti László
Department of Chemistry, Rice University , BioScience Research Collaborative, 6500 Main Street, Rm 380, Houston, Texas 77030, United States.
J Am Chem Soc. 2017 Jan 11;139(1):115-118. doi: 10.1021/jacs.6b12712. Epub 2016 Dec 23.
Herein we disclose a novel method for the facile transfer of primary (-NH) and secondary amino groups (-NHR) to heteroaryl- as well as arylcuprates at low temperature without the need for precious metal catalysts, ligands, excess reagents, protecting and/or directing groups. This one-pot transformation allows unprecedented functional group tolerance and it is well-suited for the amination of electron-rich, electron-deficient as well as structurally complex (hetero)arylmetals. In some of the cases, only catalytic amounts of a copper(I) salt is required.
在此,我们公开了一种新颖的方法,可在低温下将伯氨基(-NH)和仲氨基(-NHR)轻松转移至杂芳基铜酸盐以及芳基铜酸盐,无需使用贵金属催化剂、配体、过量试剂、保护基和/或导向基团。这种一锅法转化具有前所未有的官能团耐受性,非常适合对富电子、缺电子以及结构复杂的(杂)芳基金属进行胺化反应。在某些情况下,仅需催化量的铜(I)盐。