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Preparation of acceptors 2–4. Reagents and conditions: (i) ethylene diamine, EtOH, reflux, overnight; (ii) 4-O2NC6H4OCOCl, NaHCO3, CH3CN/H2O, rt, overnight; (iii) AcCl, DIPEA, DCM, rt, overnight; (iv) NaCNBH3, 1 M HCl in Et2O, 0 °C, 1.5 h; (v) NaH, TBAI, DMF, MS; BnBr, 2 h, rt; (vi) Troc-Cl, NaHCO3, H2O, THF.
