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(a) Methyl propiolate, CuI/DIPEA, HOAc, CH2Cl2, 0 °C to r.t., 1 h (95% yield); (b) NH3·MeOH, r.t., 48 h; (c) PPh3/I2/imidazole, CH2Cl2, 0–35 °C, 4 h; (d) DBU, THF, 65 °C, 24 h; (e) ICl/NaN3, THF, 0 °C to r.t., 8 h; (f) BzCl, DMAP, Et3N, CH2Cl2, 0 °C, 20 min; (g) m-CPBA, m-CBA, n-Bu4NHSO4/K2HPO4, CH2Cl2, 0 °C to r.t., 16 h; (h) Ni(CH3COO)2·4H2O, HOAc, reflux, 7 h; (i) NH3/MeOH, 24 h.
