2-Fluoropyrimidine as an efficient reagent in solid-phase synthesis of N-aryl- and N-alkyl-N-pyrimidin-2-ylamines

Mild and efficient reaction conditions were developed for the solid-phase synthesis of N-aryl- and N-alkyl-N-pyrimidin-2-ylamines. 2-Fluoropyrimidine in the presence of DIEA showed suitable properties for reactions with resin-bound alkylamines at room temperature. Since anilines proved to be inert under these conditions, an alternative approach was developed using BF3·Et2O as a potent catalyst for the reaction of anilines with 2-fluoropyrimidine.