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. 2021 Apr 13;12(20):7091–7097. doi: 10.1039/d1sc01174j
Entry A A′ B B′ A′ + B′
Sequence Sequence % Sequence Sequence % %
20 H-SD′LSQRG-SAL ester graphic file with name d1sc01174j-u2.jpg >98a, 48.0b Boc-(Thz)(K–S)LSQRG-SAL ester graphic file with name d1sc01174j-u3.jpg 88.9b, 37.2d 84.3b, 50.4c
21 Boc-(Thz)NFS(K–S)QSNKRFLSKTQG-SAL ester graphic file with name d1sc01174j-u4.jpg 90.1b, 35.4d 89.9b, 45.8c
a

D′ = Asp(benzofuran), (K–S) = Lys–Ser dipeptide, SAL = salicylaldehyde.

b

Percentage conversion to the ligation product based on UPLC-MS analysis of the crude reaction mixture.

c

Isolated yield based on ligation.

d

Isolated yield over 2 steps (intramolecular STL and one-pot Thz deprotection).

e

Isolated yield over 2 steps (intramolecular STL and one-pot Fmoc deprotection).