tert-Butylsulfinamide can be readily transformed into P,N-sulfinyl imine ligands through condensation with aldehydes and ketones, which can undergo iridium-catalyzed asymmetric hydrogenation of olefins. tert-Butylsulfinamide is also used as a reagent in the synthetic preparation of amide series as BACE1 inhibitor and potential anti-Alzheimer’s drug.