Monocarbonyl activation of 2,2-disubstituted malonic acids with benzotriazole leads to decarboxylation of one of the carboxy groups and formation of a CH bond. Intermediate carbonyl benzotriazoles then readily acylate nucleophilic reagents and peptides resulting in libraries of conjugates and peptidomimetics.

Polyheterocyclic pyrimidinyltheophyllines have been synthesized from pyrimidine and theophylline precursors. Attempts to cyclize these reactive bis-heterocyclic systems resulted in the formation of the corresponding diazepine moieties. In addition, modification of the reaction conditions led to the formation of imidazo[2,1-f]purines.