Scheme 1.
Schematic depiction of the syntheses of the GRPR- and NPY(Y1)R-affine HBPLs 22−26 and the scrambled analogs 24a–c. Conditions: (A) 1, H2O + 0.1% TFA, phosphate buffer, pH 4.0−4.6, RT, 5 min, yields: 47% for 17, 51% for 18, 43% for 19, 44% for 19a, 58% for 20, 55% for 21; (B) 2, H2O + 0.1% TFA, phosphate buffer, pH 4.0−4.6, RT, 5 min, yields: 82% for 22, 79% for 23, 66% for 24, 49% for 24a, 63% for 24b, 61% for 24c, 75% for 25, 73% for 26.