The chemical formation of the peptide bond has long fascinated and challenged organic chemists. It requires not only the activation of the carboxyl group of an amino acid but also the protection of the N^α-amino group. The more than a century of continuous development of ever-improved protecting group chemistry has been married to dramatic advances in the chemical synthesis of peptides that, itself, was substantially enhanced by the development of solid-phase peptide synthesis by R. B. Merrifield in the 1960s. While the latter technology has continued to undergo further refinement and improvement in both its chemistry and automation, the development of the base-labile 9-fluorenylmethoxycarbonyl (Fmoc) group and its integration into current synthesis methods is considered a major landmark in the history of the chemical synthesis of peptides. The many beneficial attributes of the Fmoc group, which have yet to be surpassed by any other N^α-protecting group, allow very rapid and highly efficient synthesis of peptides, including ones of significant size and complexity, making it an even more valuable resource for research in the post-genomic world. This review charts the development and use of this N^α-protecting group and its adaptation to address the need for more green chemical peptide synthesis processes.

长期以来，肽键的化学形成使有机化学家着迷和挑战。它不仅需要激活氨基酸的羧基，还需要保护^Nα-氨基。经过一个多世纪的不断发展，保护基团化学的不断发展与肽的化学合成取得了长足的进步，而RB Merrifield于1960年代开发了固相肽合成技术，从而大大增强了肽的化学合成。尽管后一种技术在化学和自动化方面一直在不断完善和改进，但对碱不稳定的9-芴基甲氧基羰基（Fmoc）基团的开发及其与当前合成方法的结合被认为是该技术历史上的主要里程碑。肽的化学合成。Fmoc基团的许多有益的属性，这些属性还没有被任何其它N-被超越^α-保护基，可以快速高效地合成肽，包括大小和复杂性高的肽，使其成为后基因组世界研究中更有价值的资源。这次审查的图表开发和利用这款N的^α保护基团和适应，以解决更多的绿色化学肽合成工艺的需要。