Scheme 9.
Synthetic procedure for MPUPA-(R)-isoAsp(Hda)-Gly-OH (49). Reagents and conditions: (i) DCC/HOBt, DCM/DMF, rt, 3 h; (ii) H2, Pd/C, EtOH, rt, 12 h; (iii) 20% Pip/DMF, rt, 10 min (×2); (iv) TFA/H2O/TIPS/PhOH (78:10:10:2 v/v/v/v), rt, 2.5 h.
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