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. Author manuscript; available in PMC: 2018 Sep 29.
Published in final edited form as: Eur J Med Chem. 2017 Jun 29;138:407–421. doi: 10.1016/j.ejmech.2017.06.062

Scheme 1.

Scheme 1

Reagents and conditions: (i) ClSO3H, 80 °C, 4 h, 77%; (ii) SOCl2, 80 °C, 16 h then 3,4-difluoroaniline, toluene, 110 °C, 2 h, 65%; (iii) amine, Et3N, CH2Cl2, 0 °C to rt (or 40 °C), 2 h, 26–94%.