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. 2014 Nov 13;57(23):10162–10175. doi: 10.1021/jm501568b

Scheme 1. Synthesis of the N-Arylpiperazine Compounds 3–13.

Scheme 1

Reagents and conditions: (a) 1-(aryl)piperazine, Pd(OAc)2, P(o-tolyl)3, Cs2CO3, toluene, 50 °C, 48 h, ∼60%; (b) 10% NaOH (aq), MeOH/THF (1/1), 60 °C, 3 h, >98%; (c) 15b, 16b, 17b, 18b, 19b, 20b, 21b, 22b, 23b, 24b, or 25b (as appropriate), PyBOP, HOBt, Et3N, CH2Cl2, 23 °C, 1 h, ∼60%.