Scheme 1. Synthesis of aziridine ABPs 1, 2, 3 and inhibitors 4, 5. Reagents and conditions: (a) DBBT, Et₃N, CH₂Cl₂, –78 °C, 71%; (b) (i) LiBH₄, THF, 83%; (ii) Grubbs 2^nd generation, CH₂Cl₂, 95%; (c) p-TsCl, Et₃N, CH₂Cl₂, 87%; (d) LiAlH₄, THF, 0 °C to rt, 87%; (e) (i) Li, NH₃ (l), THF, –60 °C, 73%, (ii) 2,2-dimethoxypropane, CSA, rt, 60%; (f) (i) CCl₃CN, DBU, CH₂Cl₂, rt; (ii) NaHCO₃, I₂, H₂O, rt, 46%; (g) (i) 37% HCl (aq.), MeOH, 60 °C; (ii) NaHCO₃, MeOH, rt, 65%; (h) EEDQ, benzoic acid or acetic acid, DMF, 0 °C, 7% 4, 28% 5; (i) EEDQ, 24, DMF, 0 °C 25%; (j) CuSO₄, sodium ascorbate, 25, 26 or 27, rt, 19% 1, 12% 2, 13% 3.