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. 2020 Nov 24;10(69):42457–42492. doi: 10.1039/d0ra07204d

SPPS evaluation of three solvent mixtures on Wang PS and Rink Amide ChemMatrix® resin as reported by Ferrazzano et al.41a.

Entry Peptide Solvent Resin Purity (%)
1 Aib-enkephalin DMF Wang PS 13.5
2 Aib-enkephalin DMF Rink Amide ChemMatrix® 53.0
3 Aib-enkephalin Sulfolane/DEC (3 : 7) Wang PS 72.8, 69.1b
4 Aib-enkephalin Sulfolane/DEC (3 : 7) Rink Amide ChemMatrix® 62
5 Aib-enkephalin Cyrene™/DEC (3 : 7) Wang PS 37.3, 72.0b
6 Aib-enkephalin Anisole/DMC (7 : 3) Rink Amide ChemMatrix® 72.1
7 Aib-ACP DMF Rink Amide ChemMatrix® 37.8
8 Aib-ACP Sulfolane/DEC (3 : 7) Rink Amide ChemMatrix® 10.0
9 Aib-ACP Anisole/DMC (7 : 3) Rink Amide ChemMatrix® 31.0
10 Octreotide DMF H-Thr(tBu)-ol-2CT-PS 88
11 Octreotide Anisole/DMC (7 : 3) H-Thr(tBu)-ol-2CT-PS 64.6, 82.3c, 84.9d
a

Coupling was performed for 1 h at a 0.2 M concentration using 3 equiv. of Fmoc-protected amino acid, 3 equiv. of DIC and 3 equiv. of Oxyma Pure.

b

Double coupling 2 × 1 h of the Fmoc-Leu-OH amino acid.

c

Coupling of Fmoc-Cys-OH at 40 °C.

d

Coupling for all steps at 40 °C.