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. 2022 Feb 18;15(2):245. doi: 10.3390/ph15020245

Scheme 3.

Scheme 3

Reagents and conditions:(i) 1-fluoro-2-iodoethane or 2-bromoethanol, K2CO3, CH3CN, 70 °C, 12 h; (ii) (a) NH2NH2.H2O, CH2Cl2, S8, EtOH, 50 °C, 24 h; (b) NaNO2, AcOH, 0 °C to rt, 30 min; (iii) nosyl chloride, DIPEA, DMAP, CH2Cl2, rt, 1 h; (iv) 2-fluoroethylamine or ethanolamine, CH3CN, 0 °C to rt, 12 h; (v) Boc2O, Et3N, CH2Cl2, 0 °C to rt, 12 h; (vi) HCl, dioxane, rt, 4 h; (vii) TrCl, Et3N, CH2Cl2, 0 °C to rt, 12 h.