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. 2014 Oct 1;22(19):5378–5391. doi: 10.1016/j.bmc.2014.07.043

Scheme 1.

Scheme 1

Synthetic route for 3,4,5-tri-substituted 1,2,4-triazoles. Reagents and conditions: (a) bromoethyl acetate, NaOAc in EtOH, reflux for 1 h; (b) NH2–NH2·H2O, reflux overnight; (c) (i) EtOH, reflux overnight; (ii) 1 M aq NaOH, 45 °C, 45 min then 10% aq HCl; (d) CH2Cl2, Et3N, RT, overnight; (e) K2CO3, DMF, 45 °C, overnight, then H2O.