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. Author manuscript; available in PMC: 2017 Jan 14.
Published in final edited form as: J Med Chem. 2015 Dec 30;59(1):219–237. doi: 10.1021/acs.jmedchem.5b01276

Scheme 1.

Scheme 1

Synthesis of 2-(4-fluorophenyl) and 3-(4-fluorophenyl) benzothiophene coresa

aReagents and conditions: (a) KOH, EtOH/H2O, 3-methoxythiophenol, rt, 2 h; (b) PPA, 120 °C, 3 h, 55% over two steps; (c) BF3•OEt2, DCM, rt, overnight, 73% over two steps; (d) BBr3, DCM, −78 °C to rt, overnight.