Synthesis of 3,5,7-Trisubstituted Indoles
Jonathan Sperry describes an Ir-catalyzed C–H borylation approach to synthesize trisubstituted indoles.
Synthetic Access to 3,5,7-Trisubstituted Indoles Enabled by Iridium-Catalyzed C–H Borylation: A. S. Eastbrook, J. Sperry
Synthesis 2017, 49, DOI: 10.1055/s-0036-1589018
Indole rings are widespread among drugs, natural and bioactive compounds. For this reason, indoles having diverse substitution patterns represent targets of great interest for organic chemists. The 3,5,7-substitution pattern is not frequently encountered in the literature, but it represents a very interesting option for the development of novel bioactive compounds. Professor Jonathan Sperry (University of Auckland, New Zealand) has recently described a new strategy for accessing 3,5,7-substituted indoles.
Synthetic approach to 3,5,7- trisubstituted indolesvergrößern
Professor Sperry said: “In a cyclization-free approach to heteroaromatic construction, indoles harboring a rare substitution pattern are attainable using an iridium-catalyzed triborylation–protodeborylation sequence.”