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. Author manuscript; available in PMC: 2022 Sep 26.
Published in final edited form as: Bioorg Med Chem Lett. 2020 Sep 12;30(24):127543. doi: 10.1016/j.bmcl.2020.127543

Scheme 1.

Scheme 1.

Synthesis of 8 – 18. Reagents and conditions: (a) EDC•HCl, HOBt or HOAt or DMAP, TEA or DIPEA, DMF or DCM, rt or 0 °C to rt, 16 h, 17–80%. (b) i) oxalyl chloride, DMF (cat.), DCM, rt. ii) aniline, TEA, rt, 6 h, 40%. (c) MeI, K2CO3, acetone, rt, 16 h, 64%. (d) 10% Pd/C, H2 (1 atm), EtOAc, rt, 3 h, 34%.