Nitrogen-containing heteroarenes are present in 11 of the top 25 most frequently occurring ring systems in U.S. approved drugs. Of these, Lewis basic azines, such as pyridines, pyrimidines, quinazolines and pyrazines, are some of the most prevalent structural units and share the unique properties that make this type of aromatic heterocycle an attractive component in drug molecules -namely, hydrogen bond-acceptor ability and the capacity to interact via nonpolar interactions. Moreover, the nitrogen atom in azine ring systems can confer considerable improvement of key pharmacological parameters, including biochemical potency, binding affinity, aqueous solubility and metabolic stability. The presentation of an azine feature connected through the 2-position to an alkylamine substituent -a so-called α-alkyl 2-azinyl amine -represents an attractive polar scaffold in the design of pharmaceutical and agrochemical candidates due to the density of polar functionality, multiple diversification points for analogue synthesis and a balance of C(sp ) and C(sp 2 ) carbon frameworks.