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Reagents and conditions: (a) 25% piperidine, DMF, 30 min; (b) hydrocinnamaldehyde, 2,6-dimethylphenyl isocyanide, (R)-( + )-2-bromopropionic acid, MeOH/CHCl3 (1/4), RT, 2 × 2 h; (c) 25% TFA/DCM; (d) 10% DIPEA, DCM, 18 h; (e) Boc-Phe-OH, NMM, isobutyl chloroformate, THF, DMF; (f) 25% TFA/DCM; (g) 2 M AcOH, IPA, 50 °C, 18 h.
