Scheme 1.
The solid-phase peptide synthesis (SPPS) strategy on the example of peptides 3 and 4: (a) 20% piperidine in DMF; (b) 2 eq Fmoc-Dhp-OH, HATU, and DIPEA; (c) 2 eq Fmoc-Dab(Boc)-OH, HATU, and DIPEA; (d) 2 eq Fmoc-Lys(Alloc)-OH, HATU, and DIPEA; (e) 2 eq Boc-Lys(Fmoc), HATU, and DIPEA; (f) 2 eq Fmoc-Cys(Trt)-OH, HATU, and DIPEA; (g) Pd(PPh3)4 and PhSiH3; (h) 2 eq Fmoc-hArg(Pbf)-OH, HATU, and DIPEA; and (i) TFA:DTT:H2O:TIS.
