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Reagents and conditions: (a) Hydroxymethyl polystyrene resin, Ph3P, diethyl azodicarboxylate, THF; (b) TFA/DCM, 1 h; (c) OHCCO2H·H2O, R4B(OH)2, DCM; (d) DIC, R5NH2, DCM; (e) 25% piperidine in DMF; (f) Boc-AA-OH, (benzotriazol-1-yloxy)tripyrrolidinophosphonium hexafluorophosphate (PyBOP), DMF; (g) 2% TFA in DCM, 1 h; (h) 2 M AcOH, iBuOH, 50 °C, 24 h.
