Sivanandaiah K M, Babu V V, Renukeshwar C
Department of Studies in Chemistry, Central College, Bangalore University, India.
Int J Pept Protein Res. 1992 Mar;39(3):201-6. doi: 10.1111/j.1399-3011.1992.tb00789.x.
Fmoc-amino acid chlorides were employed in the solid phase synthesis of the opioid peptides [Leu]enkephalin, [Leu]enkephalin amide, and dermorphin. The conventional polystyrene-based Merrifield resin or Wang's resin served as solid support. A binary salt of either triethylamine or diisopropylethylamine in the presence of 1-hydroxybenzotriazole or pivalic acid was used for acylation. The coupling rates were quite fast, being comparatively faster when 1-hydroxybenzotriazole was used along with triethylamine or diisopropylethylamine. The peptides obtained in good yields showed, after purification, biological and spectral properties identical with those of the natural peptides.
芴甲氧羰基氨基酸氯化物被用于阿片样肽[亮氨酸]脑啡肽、[亮氨酸]脑啡肽酰胺和皮啡肽的固相合成。传统的基于聚苯乙烯的 Merrifield 树脂或 Wang 树脂用作固相载体。在 1-羟基苯并三唑或新戊酸存在下，使用三乙胺或二异丙基乙胺的二元盐进行酰化。偶联速率相当快，当 1-羟基苯并三唑与三乙胺或二异丙基乙胺一起使用时相对更快。纯化后得到的肽产率良好，其生物学和光谱性质与天然肽相同。
