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. 2022 Apr 28;65(17):11574–11606. doi: 10.1021/acs.jmedchem.2c00252

Scheme 1. Synthesis of Derivatives 5a–5e, 6a–6d, 7a–7e, and 8a.

Scheme 1

Reagents and conditions: (a) piperidine, DCM, room temperature (r.t.), 30 min. (93–99%); (b) Boc2O, TEA, DMAP, DCM, r.t., 12 h (70%); (c) Zn, AcOH, r.t., 1 h (98–99%; (d) DCC, DMAP, DCM, r.t., 8–12 h (80–88%); (e) DCM/TFA, 9:1, r.t., 1 h (60–99%); (f) TEA, DMAP, DMF, r.t., 24 h (30–85%); (g) LiOH, MeOH/H2O, r.t., 48 h (80–92%); (h) phenyl chloroformate, TEA, EtOAc, r.t., 12 h (70%); (i) TEA, DMF, r.t., 24 h (80–87%).