American Chemical Society
ol9b01501_si_001.pdf (3.58 MB)

Synthesis of 2‑Aminoindoles through Gold-Catalyzed C–H Annulations of Sulfilimines with N‑Arylynamides

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journal contribution
posted on 2019-05-20, 15:37 authored by Xianhai Tian, Lina Song, Matthias Rudolph, Frank Rominger, A. Stephen K. Hashmi
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 α-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.