Cyclobutanes are privileged four-membered synthetic targets because they are versatile skeletons of natural products and pharmaceuticals with diverse biological properties, and also serve as key intermediates in the synthesis of structurally complex molecules. Among these, cyclobutyl amines stand out as pivotal cores in medicinal development, which can be found in a large variety of bioactive molecules, as illustrated in Scheme 1A. Therefore, the development of novel strategies for synthesizing cyclobutyl amines, preferably with stereocontrol, would not only enrich the toolkit of synthetic chemists but also significantly expand the compound library available for drug discovery. In addition to the well-established [2+2] cycloaddition strategy, the strain-release reaction of bicyclo[1.1.0]butanes (BCBs) has emerged as an alternative for synthesizing different types of cyclobutanes. Despite impressive progess, developing modular strategies for the synthesis of cyclobutyl amines, especially with stereocontrol and molecular complexity, remains challenging. To meet this challenge, three innovative protocols have been developed. In 2016, Baran and co-workers reported a "strainrelease amination" strategy (Scheme 1A, top). This method utilized BCB sulfones as electrophiles in reactions with various amine nucleophiles to construct 3-sulfonyl cyclobutylamines. Controlling cis/trans selectivity was difficult, resulting in poor stereocontrol during late-stage transformations. The direct removal of the arylsulfonyl group reduced molecular complexity. Besides, Aggarwal and co-workers developed a BCB-boronate complex from the corresponding lithiated BCB and boronic ester. This complex enabled an appealing difunctionalization of the central C-C σ-bond with various electrophiles including imines (Scheme 1B, middle). In this case, the generation of lithiated BCB required the use of hazardous tert-butyl lithium, and only two examples of cyclobutyl methanamines were presented albeit with good diastereoselectivity. Recently, Leitch and co-workers realized an elegant Lewis acid-catalyzed reaction of BCB esters with N-alkyl or N-aryl imines for the divergent synthesis of cyclobutenyl methanamines (via E1 elimination) and azabicyclohexanes (aza-BCHs, via nucleophilic attack), respectively (Scheme 1C, bottom). Both products were formed in parallel pathways that share a common Leitch's carbocation intermediate derived from the C-C bond formation between the Lewis acid activated BCB enolate species and the imine. Thus, the cyclobutenyl methylamines typically achieved low to moderate yields due to the competitive aza-BCHs.