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. Author manuscript; available in PMC: 2021 Mar 24.
Published in final edited form as: J Med Chem. 2020 Apr 22;63(10):5242–5256. doi: 10.1021/acs.jmedchem.0c00035

Scheme 4.

Scheme 4.

Synthesis Procedure of Series IIIa aReagents and conditions: (a) 50% KOH, EtOH, rt, overnight, used directly for next step. (b) I2, DMSO, 140 °C, 4 h, 36%. (c) Pd(PPh3)4, K2CO3, CH3OH, 90 °C, 7 h, 75%. (d) R4–Br, K2CO3, DMF, 80 °C, overnight, 55–72%. (e) R5–H, K2CO3, DMF, 80 °C, overnight, 18–65% for two steps. (f) DAST, CH2Cl2, rt, overnight, 80%.