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. Author manuscript; available in PMC: 2023 Apr 20.
Published in final edited form as: J Med Chem. 2021 Dec 15;64(24):18025–18053. doi: 10.1021/acs.jmedchem.1c01382

Scheme 2a.

Scheme 2a

aReagents and conditions: (a) HCl/Et2O, rt, overnight; (b) (COCl)2, 160 °C, 2.5 h; (c) NaOH, H2O2, 80 °C, 0.5 h; (d) ammonium hydroxide, HOBt, EDCI, NMM, THF, overnight, rt; (e) benzaldehyde derivatives, DMAC, PTSA, NaHSO3, 120 °C, 4–8 h.