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. 2021 Feb 6;26(4):867. doi: 10.3390/molecules26040867

Scheme 1.

Scheme 1

Reagents and conditions: (i) diethyl 2-oxomalonate (1 eq), citric acid (15 mol%), EtOH, rt, 2–24 h, 16–54%; (ii) N,N-dimethylformamide (DMF) (cat.), POCl3, 0 °C, and then reflux, 3 h, 51–100%; (iii) 3-aminophenol (1.1–3 eq), EtOH, MW 150 °C, 3 h, 29–99%; (iv) 3-aminophenol (3 eq), p-toluenesulfonic acid (cat.), EtOH, MW 100 °C, 8 h, 70%; (v) K2CO3 (3 eq), MeOH/H2O (4/1), reflux, 4 h, 94–100%.