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. 2012 Apr 23;55(9):4244–4273. doi: 10.1021/jm300041e

Scheme 3. Modification on the 6 Position of Imidazolopiperazine Core.

Scheme 3

Reagents and conditions: (a) methallyl chloride, K2CO3, KI, DMF, rt, 55%; (b) AcOH/MsOH (6:1), 210 °C, 39%; (c) N-Boc-glycine, HATU, DIEA, DMF, rt; 57%; (d) Br2, AcOH, CH2Cl2, rt; 55%; (e) ArNH2, Pd2(dba)3, xantphos, Cs2CO3, dioxane, 150 °C; (f) TFA, CH2Cl2, rt, 55% over 2 steps (for example 25, Ar = 4F-Ph).