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. Author manuscript; available in PMC: 2018 Dec 28.
Published in final edited form as: ChemMedChem. 2016 Mar 16;11(16):1709–1720. doi: 10.1002/cmdc.201600015

Scheme 1. Synthetic route to cHTCs.

Scheme 1.

Reagents and conditions: a) ammonium acetate, glacial acetic acid, benzene, reflux, 16 h; b) sulfur, N,N-diethylamine, 40–50 °C, 1.5 h, the two steps 25–59%; c) R1COCl, dry pyridine, 2–72 h, 7–49%; d) 10% Pd/C, ammonium formate, MeOH/DMF, rt, 1–120 h, 30–80%; e) BBr3, dry CH2Cl2, rt, 2 h, 19–60%.