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. 2014 Dec 12;6(2):204–209. doi: 10.1021/ml5004475

Scheme 2. Synthesis of Aromatic-Containing Lactams.

Scheme 2

Reagents and conditions: (a) EDCI, DMAP, Et3N, THF, rt, 12 h, 80%; (b) LiOH·H2O, MeOH/THF/H2O, rt, 12 h, 95%; (c) NaOAc, Ac2O, 110 °C, 3 h, 60%; (d) K2CO3, MeOH, 2 h, 85%; (e) 6, NaH/K2CO3, DMF, 12 h, 20–70%; (f) 10% Pd/C, H2, AcOH, MeOH/EtOAc, rt, 2–3 d, 20–60%.