The first total synthesis of the natural nematicidal cyclic lipodepsipeptide ophiotine via a convergent strategy that involved both solid-phase peptide synthesis and liquid phase chemistry is reported. The pre-made dipeptide building block was synthesized in the liquid phase, which was then assembled into the peptide backbone through standard Fmoc chemistry on solid support. After cleavage from the resin, the linear peptide was cyclized by the liquid phase macrocyclization and the side chain deprotection successively, which led to the crude ophiotine. Finally, the crude product was purified by preparative reverse-phase highperformance liquid chromatography, and its structure was confirmed by NMR and HR-ESI-MS.

中文翻译：

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环状脂缩酚肽的全合成

报道了通过涉及固相肽合成和液相化学的收敛策略首次全合成天然杀线虫环脂缩肽鱼碱。预制的二肽构建块在液相中合成，然后通过固体支持物上的标准 Fmoc 化学组装成肽主链。从树脂上裂解下来后，线性肽依次通过液相大环化和侧链脱保护环化，得到粗品蛇麻碱。最后，粗产物经制备型反相高效液相色谱纯化，其结构经NMR和HR-ESI-MS确证。