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. Author manuscript; available in PMC: 2022 Aug 12.
Published in final edited form as: J Med Chem. 2021 Aug 3;64(15):11729–11745. doi: 10.1021/acs.jmedchem.1c01136

Scheme 2. Synthesis of Piperidine “C-linked” Analogs.

Scheme 2.

Reagents and conditions: (a) Cs2CO3, Pd((t-butyl)3P)2, toluene: EtOH: H2O (9:3:1), 120 °C, overnight, 30-35% (b) 10% Pd/C, 60 psi, CH3OH, 16 h, 80%, (c) 4M HCl in dioxane 89-98%, (d) DIEA,3,4-dichloroisocyanate, DMF, 10-45% (e) DIEA, EDCI, HOBT, 3,4-dichlorophenylacetic acid, DMF, 30-85%