Synthesis of 2-Aminoindoles through Gold-Catalyzed C–H Annulations of Sulfilimines with <i>N</i>-Arylynamides
作者:Xianhai Tian、Lina Song、Matthias Rudolph、Frank Rominger、A. Stephen K. Hashmi
DOI:10.1021/acs.orglett.9b01501
日期:2019.6.7
A new gold-catalyzed C-H annulation of sulfilimines with N-phenylynamides is presented. As key intermediates of this operationally simple reaction, the in situ generated a-imino gold carbenes insert into the ortho C-H bonds of the phenyl groups to afford 2-aminoindoles bearing a variety of substitution patterns in high selectivities. This reaction offers a facile approach to biologically important 2-aminoindoles by using inexpensive and readily available starting materials.