Backbone-fluorinated amino acids exhibit unique conformational behaviour, and have potential utility as components of bioactive shape-controlled peptides. However, methods for the elaboration of backbone-fluorinated amino acids have thus far been limited to solution phase peptide coupling reactions. In this paper, protocols are developed that allow the successful manipulation of backbone-fluorinated amino acids using Fmoc-strategy solid phase peptide synthesis. To exemplify this strategy, several fluorinated RGD peptide analogues were synthesised in moderate to good overall yields.
骨架
氟化
氨基酸表现出独特的构象行为,具有作为
生物活性形状控制肽成分的潜在用途。然而,迄今为止,骨干
氟化
氨基酸的制备方法仅限于溶液相肽链偶联反应。本文开发的方案允许使用 Fmoc 策略固相肽合成法成功操作骨架
氟化
氨基酸。为了说明这种策略,我们合成了几种
氟化 RGD 肽类似物,总产率从中等到良好。