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

Scheme 3. Synthesis of Derivatives 911.

Scheme 3

Reagents and conditions: (a) proper N-protected amino acid, DCC, DMAP, DCM, r.t., 8–12 h (79–81%); (b) piperidine, DCM, 30 min (72–99%); (c) DCM/TFA, 9:1, r.t., 1 h (68–74%); (d) 4-methoxyphenyl isocyanate, TEA, THF, r.t., 4 h (79–82%); (e) DCM/TFA, 1:9, r.t., 24 h (68–77%).