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DOTA-D-Ala-D-Lys(HSG)-D-Glu-D-Lys(HSG)-NH2[ No CAS ]
Yield
Reaction Conditions
Operation in experiment
The peptide was synthesized (NB Ref. CN 2-34) by solid phase peptide synthesis on Rink Amide resin (2.0159 g, 0.7 mmol/g) using standard Fmoc synthesis methodology. The following amino acids (6 equivalents per coupling) were added in the order shown; Fmoc-D-Lys(Aloc)-OH, Fmoc-D-Glu(OBut)-OH, Fmoc-D-Lys(Aloc)-OH, Fmoc-D-Ala-OH and DOTA-tris(t-Butyl) ester. Each amino acid was double coupled with two hour couplings first using diisopropylcarbodiimide followed by a coupling using O-Benzotriazole-N,N,N',N'-tetramethyl-uronium-hexafluoro-phosphate (HBTU) as the activating agents. The Aloc side chains were then removed with the Pd catalyst in the usual way and the trityl-HSG-OH was double coupled to the lysine side chains. The peptide was cleaved from the resin with TFA, precipitated in ether, and purified by HPLC to obtain the desired peptide. Successful synthesis was confirmed by ESMS analysis, MH+: 1361. The total yield of desired product was 298.8 mg in 6 fractions. Out of these 6 fractions, 4 contain pure peptide amounting to 201.3 mg while the remaining two fractions contain a slight impurity with a total mass of 97.5 mg.
DOTA-D-Glu-D-Lys(HSG)-D-Glu-D-Lys(HSG)-NH2[ No CAS ]
Yield
Reaction Conditions
Operation in experiment
The peptide was synthesized by solid phase peptide synthesis on Sieber Amide resin using the Fmoc procedure. The following amino acids were added in the order shown; Fmoc-D-Lys(Aloc)-OH, Fmoc-D-Glu(OBut)-OH, Fmoc-D-Lys(Aloc)-OH, Fmoc-D-Glu(OBut)-OH, DOTA-tris(tBu) ester. Each amino acid was double coupled with two hour couplings first using diisopropylcarbodiimide followed by a coupling using O-Benzotriazole-N,N,N',N'-tetramethyl-uronium-hexafluoro-phosphate (HBTU) as the activating agents. The Aloc side chains were then remove with the Pd catalyst in the usual way and the trityl-HSG-OH was double coupled to the lysine side chains. The peptide was cleaved from the resin with TFA, precipitated in ether, and purified by HPLC to obtain the desired peptide