1505566-40-4Relevant academic research and scientific papers
Synthesis of pyridopyrimidines by palladium-catalyzed isocyanide insertion
Estevez, Veronica,Van Baelen, Gitte,Lentferink, Babette H.,Vlaar, Tjostil,Janssen, Elwin,Maes, Bert U. W.,Orru, Romano V. A.,Ruijter, Eelco
, p. 40 - 43 (2014)
A new synthetic approach to 4-aminopyrido[2,3-d]pyrimidines and 4-aminopyrido[3,2-d]pyrimidines based on palladium-catalyzed reaction of isocyanides with readily available N-(bromopyridyl)amidines is reported. The target heterocycles were obtained in generally good to excellent yield. For the two regioisomeric pyrimidopyrimidines, we compared our approach involving oxidative addition with the analogous C-H activation protocol because both methods have been reported for the synthesis of 4-aminoquinazolines. We found that the C-H activation protocol does not allow one to obtain the target pyridopyrimidines, but the imidoylative cross-coupling protocol provided a new entry to the synthesis of these medicinally important scaffolds.
