Table 1. Selected examples of linear peptide (A) cyclization leading to macrocyclic (B) and amidine-based products (C and D).
| ||
Linear peptide (A) | Sequence | Major product isolated yield |
14 | PGLGF | 34% B45 |
15 | PGlGF | 28% B |
16 | PALGF | 12% B |
17 | PGLAF | 9% B a |
18 | PGLGf | 12% C |
19 | PS(tBu)LGF | 49% B b |
20 | PS(tBu)LY(tBu)F | 22% B |
21 | PGLGK(Boc) | 23% B a |
22 | PGlGk(Boc) | 8% D a |
23 | PGLK(Boc) | 8% D a |
24 | PGF | 8% C |
aIsolated after telescopic synthesis.
bCyclized with d-leucine-derived dimer.