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Reagents and conditions: (a) p-TsCl, TEA, DMAP, DCM dry, rt, 22 h; (b) Cs2CO3, ACN dry, N2, 60 °C, 18 h - 3 days; (c) H2, Pd/C, EtOAc, CH3CO2Na, rt, 3 h; (d) HATU, TEA, DCM dry, N2, rt, 3 h; (e) TFA/DCM 1.7:10, rt, 1 h.
