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Reagents and Reaction Conditions: (a) EDCI·HCl, HOBt, DMF, DIEA, 3-aminopropionitrile, r.t., 15 h, (95%); (b) (i) PPh3, DIAD, TMSN3, 0 °C, 30 min, then r.t., 2 h, then 50 °C, 17 h; (ii) DBU, CH2Cl2, r.t., 6 h, (63%); (c) NH2OH·HCl, DMSO, 90 °C, 3.5 h, (61%); (d) NaN3, ZnBr2, H2O, 150 °C, 24 h, (20%).
