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. Author manuscript; available in PMC: 2022 Apr 22.
Published in final edited form as: J Med Chem. 2021 Mar 31;64(8):5099–5122. doi: 10.1021/acs.jmedchem.1c00164

Scheme 3. Synthesis of Triazole-Containing Derivatives with Cyclic Replacement of the Piperidine Ring of 3aa.

Scheme 3.

aReagents and conditions: (a) Pd(PPh3)4, K2CO3, DMF, 85 °C, 5 h, and 46–91%; (b) Pd(PPh3)4, K2CO3, DMF, μW, 100 °C, 0.5 h, and 80–91%; (c) Pd(PPh3)4, K2CO3, DMF/H2O = 1:1, 90 °C, 12 h, and 30–70%; (d) KOH, MeOH/H2O = 2:1, 50 °C, and 43–74%; and (e) TFA/THF = 2:1, rt, 0.5 h, and 52–90%.