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. 2018 Oct 19;9(12):1205–1210. doi: 10.1021/acsmedchemlett.8b00371

Scheme 1. General Route 1 for Synthesis of Pyrazole Quinolones.

Scheme 1

Conditions and reagents: (a) pyrazole boronic acid pinacol ester, 10 mol % PdCl2(dppf), K2CO3·1.5H2O, dioxane, reflux, 24 h; (b) AcOH, H2O, 120 °C, 24–48 h or HCl(aq), dioxane, reflux, 48 h or HCOOH/H2O, DMF, 140 °C, 4 h; (c) sodium dichloroisocyanurate, MeOH, NaOH(aq), r.t., o/n.