Scheme 1.
Syntheses of [nat/67Ga]Ga-DOTA-(linker)-IPLPPPRRFFFK (linker = none, aaa, aaaaa, ββ, ββββ, EG2, EG4). Reagents and conditions: (a) 30% HFIP, rt, 5 min; (b) DIPEA, DMF, rt, overnight; (c) 95% TFA, 2.5% triisopropylsilane, 2.5% H2O, rt, 2 h; (d) Ga(NO3)3, H2O, 40 °C, 4 h; (e) [67Ga]GaCl3, 2 M HEPES pH 5.0, 85 °C, 10 min.