Table 2.
Peptide | Cycle | |||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
1 | 2 | 3 | 4 | 5 | 6 | 7 | 8 | 9 | 10 | 11 | 12 | 13 | 14 | 15 | 16 | |
CSP1 | A | A | A + B | A + B | A + A + B + C | A + A | A + A | A + A | A + A | A + A + B + C | A + A | A + A | A + A | A + A | A + A + B + C | A + A + C |
AcCSP1 | A | A | A + B | A + B | A + A + B + C | A + A | A + A | A + A | A + A | A + A + B + C | A + A | A + A | A + A | A + A | A + A + B + C | A + A + C |
Ac4CSP1 | A | A | A + B | A + B | A + A + B + C | A + A | A + A | A + A | A + A | A + A + B + C | A + A | A + A | A + A | A + A | A + A + B + C | A + A + C |
CSP1hβE | D | D | D | D + C | E + C | E | E | E | E | C | E | E | E | C + E | C | C |
CSP1AA | F | F | F | C | C | F | F | F + F | C | C | F | C | C | C | C | C + C |
CSP1Y(SO3) | D | D | D | D + C | E + C | E | E | E | E | C | E | E | E | C + E | C | C |
(A) single coupling with 5eq. AA, 5eq. 0.45M HBTU/HOBt in DMF, 10eq. 2M DIPEA in NMP; (B) single coupling with 5eq. AA, 5eq. 0.45M HATU/HOAt in DMF, 10eq. 2M DIPEA in NMP; (C) single coupling with 8eq. AA, 8eq. 0.95M PyOxym in DMF, 16eq. 2M DIPEA in NMP; (D) single coupling with 5eq. AA, 10eq. 0.95M PyOxym in DMF, 16eq. 2M DIPEA in NMP; (E) single coupling with 10eq. AA, 10eq. 0.95M PyOxym in DMF, 16eq. 2M DIPEA in NMP; (F) single coupling with 5eq. AA, 5eq. 0.95M PyOxym in DMF, 10eq. 2M DIPEA in NMP.