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Reagents and conditions: (a) 1,2-Dibromoethane, tetramethylguanidine, DMF, 60 °C; (b) Fmoc SPPS; (c) HCO2H neat, 60 °C, 3 h; (d) Pd(PPh)3, PhSiH3, DCM, 2 × 30 min; (e) H-Pro-OMe HCl, PyBOP, DIPEA, DCM; (f) 20% piperidine/DMF; (g) TFA/3,5-dimethoxybenzene/DCM (0.5/0.5/9); (h) aryl halides, Pd(OAc)2, AgBF4, 2-NO2-Bz, PBS/DMF (1/1), MW 80 W, 80 °C, 15 min.
