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Reagents and reaction conditions: i) AA-OMe (1.5–1.7 eq.). HATU (2.0 eq.), DIPEA (6.0 eq.), DMF, 60°C, 30 min. ii) water, MW, 160°C, 70 min. iii) R3-NH2 (1.7–2.0 eq.), PEMB (1.0 eq.), glacial acetic acid (2.3–2.6 eq.), MeOH, r.t. o.n.
