Synthetic route for the preparation of lead peptide 1. a Pd(PPh3)4, K3PO4 [DMA], 80 °C, 22 h, argon; b H-L-homoPhe-RACM, PyBOP, HOAt, DIPEA [DMF/DCM], r.t., 24 h; c TFA/TIPS/H2O; d tetraalkylammonium carbonate [THF], r.t., 2 h; e HOAt, DIC [DMF/DCM], r.t., 19 h; f TFA/TIPS/H2O. Detailed synthesis procedures are given in the supporting information