Copper-Catalyzed Intramolecular C–H Amination: A New Entry to Substituted Xanthine DerivativesWe gratefully acknowledge financial support by a Grant-in-Aid for Scientific Research (C) (No. 16K08187) from the Japan Society for the Promotion of Science.
Received: 19 March 2017
Accepted after revision: 10 April 2017
09 May 2017 (eFirst)
Published as part of the Special Topic Modern Cyclization Strategies in Synthesis
Catalytic synthesis of xanthines was achieved in the presence of a copper catalyst. The process involves copper-catalyzed intramolecular C–H amination of benzamidines that possess a uracil moiety and produces variously substituted xanthines generally in good to high yields. This work introduces a new, facile approach to polysubstituted xanthine compounds.