Cu/base co-catalyzed [3+3] cycloaddition for the synthesis of highly functionalized 4-fluoropyridines

An efficient, straightforward and general method for the de novo synthesis of highly functionalized 4-fluoropyridines was developed via a cooperative copper- and base-catalyzed [3+3] cycloaddition of active methylene isocyanides with difluorocyclopropenes. The resulting 4-fluoropyridines can be readily diversified by various nucleophiles.