Scheme 3. Fmoc-solid-phase peptide synthesis of tikitericin 1. Reagents and conditions: (a) DIC, Fmoc-Leu-HMPP, CH₂Cl₂, 24 h; (b) Fmoc-SPPS: (i) PyBOP, 6-Cl-HOBt, NMM, DMF, 40 min; (ii) 20% piperidine in DMF (v/v), 2 × 5 min; (c) Pd(PPh₃)₄, PhSiH₃, DMF/CH₂Cl₂ (v/v, 1/1), 2 h; (d) 20% piperidine in DMF (v/v), 2 × 5 min; (e) PyBOP, 6-Cl-HOBt, NMM, DMF, 2 h; (f) TFA/H₂O/TIPS (v/v/v, 95/2.5/2.5), 1 h; (g) TFA/H₂O/TIPS/EDT (v/v/v/v, 94/2.5/2.5/1), 1 h. TIPS, triisopropylsilane; EDT, 1,2-ethanedithiol.