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. Author manuscript; available in PMC: 2016 May 23.
Published in final edited form as: J Med Chem. 2013 Nov 11;56(22):9045–9056. doi: 10.1021/jm400904m

Scheme 1.

Scheme 1

aSynthetic Scheme towards screening hit and analogs.

aReagents and conditions. a) EtOH, CHCCH2Br, reflux, 47% yield; b) Pd(PPh3)4, CuI, DMF, rt, 72% yield; c) TMSI, toluene; d) py, Et3N, PPh2I; e) 30% H2O2, 30–50% yield over 2 steps; f) sulfur, 30–50% yield over 2 steps; g) Me2SO4, 1,4-dioxane, sealed tube, 100–120 °C, 30–50% yield.