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Reagents and conditions: (a) Ac2O, reflux, 12 h, 76%–85%; (b) Et3N, 4-DMAP, DCM, rt, 8 h, 64%–75%; (c) HATU, DIEA, DMF, rt, 12 h, 64%–85%; (d) 10% Pd/C, H2, MeOH, rt, 2 h, 89%–96%; (e) O-tritylhydroxylamine, HATU, DIEA, DMF, rt, 12 h, 62%–79%; (f) TES, 20% TFA/DCM, rt, 30 min, 71%–84%.
