Accordingly, the α-alkyl 2-azinyl amine motif can be found in a variety of biologically and medicinally relevant molecules (Fig. ). For example, introduction of the α-amine moiety to a 2-alkyl-pyrimidine scaffold enabled improved physical properties and cell permeability for an inhibitor of human immunodeficiency virus type-1 (HIV-1) integrase, which led to the identification of a potentially clinically useful antiretroviral agent. Despite broad interest in the α-alkyl 2-azinyl amine feature, the availability of surprisingly few general and concise methods for their preparation appears to have hindered their wider utilization.