A convergent and efficient transition-metal-free catalytic synthesis of 2-aryl-indoles has been developed. The interception of a highly reactive and transient aza-ortho-quinone methide by an acyl anion equivalent generated through N-hetereocyclic carbene catalysis is central to this successful strategy. High yields and a wide scope as well as the streamlined synthesis of a kinase inhibitor are reported.
A convergent and efficient transition-metal-free catalytic synthesis of n class="Chemical">2-aryl-indoles has been developed. The interception of a highly reactive and transient aza-ortho-quinone methide by an acyl anion equivalent generated through N-hetereocycliccarbene catalysis is central to this successful strategy. High yields and a wide scope as well as the streamlined synthesis of a kinase inhibitor are reported.
Authors: Alexey Kuznetsov; Anton Makarov; Aleksandr E Rubtsov; Alexander V Butin; Vladimir Gevorgyan Journal: J Org Chem Date: 2013-11-20 Impact factor: 4.354