Scheme 1a.
aReagents and conditions: (a) tert-butyl-1,3-diisopropylisourea, CH2Cl2, rt, 3 d; (b) carbonyldiimidazole, CH2Cl2, rt, 1 h; (c) l-glutamic acid di-tert-butyl ester, neat, 45 °C, 2 d; (d) TFA/CH2Cl2 (1/1), rt, 2 h; (e) N-succinimidyl-4-fluorobenzoate or N-succinimidyl-4-[18F]fluorobenzoate, Et3N, DMSO, rt, 2 h; (f) N-succinimidyl-4-iodobenzoate or N-succinimidyl-4-[125l]iodobenzoate, diisopropylethylamine, DMSO rt, 1 h.