Forino R, Galantino M, Ciprandi F, Baumer L, Arlandini E, De Castiglione R
Farmitalia Carlo Erba S.r.l., Research and Development, Nerviana (MI), Italy.
Int J Pept Protein Res. 1994 Jun;43(6):513-9.
The impurities which formed in the large-scale synthesis of THF-gamma 2, an immunomodulatory peptide of formula H-Leu-Glu-Asp-Gly-Pro-Lys-Phe-Leu-OH, were identified by a combination of analytical methods, and their structure confirmed by synthesis. Most impurities originated from side-reactions involving the aspartyl residue (cyclization, beta-aspartyl formation and cleavage). Based on this knowledge, modifications were introduced into the work up and the purification procedure which resulted in a very pure final product (> 99% by RP-HPLC).
通过多种分析方法鉴定了在大规模合成THF-γ 2（一种化学式为H-Leu-Glu-Asp-Gly-Pro-Lys-Phe-Leu-OH的免疫调节肽）过程中形成的杂质，并通过合成确认了其结构。大多数杂质源于涉及天冬氨酰残基的副反应（环化、β-天冬氨酰形成和裂解）。基于这一认识，对后处理和纯化程序进行了改进，从而得到了非常纯的最终产物（通过反相高效液相色谱法测定纯度>99%）。
