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. 2015 Jul 27;6(9):977–981. doi: 10.1021/acsmedchemlett.5b00159

Scheme 1. Synthesis of Compounds 5a5w.

Scheme 1

Reagents and conditions: (a) 1,1,1,5,5,5-hexafluoropentane-2,4-dione, acetic acid, and sulfuric acid, reflux, 12 h, 63%; (b) methyl bromopyruvate, acetone, reflux, 12 h, 38%; (c) LiOH, THF/H2O (v/v: 1:1), 50 °C, 6 h, 90%; (d) amine component, HATU, DIPEA, DMF, r.t., 1–6 h, 15–68%.