In this paper, a series of novel tri(4-benzoylphenyl) phosphate derivatives with unique precipitation-inducing properties were synthesized and used as C-terminal supports for peptide synthesis. Mediated and assisted by tri(4-benzoylphenyl) phosphate derivatives, intermediate and target peptides could be separated conveniently via precipitation, which was likely to occur and was conducive to the rapid purification of the intermediates of peptide synthesis without the time-consuming and high-cost process of chromatographic separation and/or recrystallization. Based on these small-molecule supports, both Fmoc and Boc strategies for efficient peptide synthesis via the processes of liquid reaction and solid precipitation were proposed and demonstrated. Due to the peptide synthesis supports developed herein combined with the higher loading performance (loading value 3 mol/1 mol support) and the easily recyclable nature, and the processes of liquid reaction and solid precipitation combining the merits of both liquid-phase peptide synthesis and solid-phase peptide synthesis, a high-yielding, scalable, atom-economical and environment-friendly method of peptide synthesis was developed. The innovative method holds great promise in the fields of organic chemistry and chemical biology research, especially in peptide-based biomedical material and drug synthesis.

中文翻译：

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磷酸三（4-苯甲酰基苯基）酯（TBP）衍生物作为小分子载体介导的无树脂肽合成

本文合成了一系列具有独特的沉淀诱导特性的新型三（4-苯甲酰基苯基）磷酸酯衍生物，并将其用作肽合成的C端载体。在磷酸三（4-苯甲酰基苯基）衍生物的介导和辅助下，中间体和目标肽可通过沉淀方便地分离，这很可能发生，并且有助于快速纯化肽合成中间体，而无需耗时且费用高昂。色谱分离和/或重结晶的成本过程。基于这些小分子支持，Fmoc和Boc策略均可通过提出并证明了液相反应和固体沉淀过程。由于本文开发的肽合成载体具有更高的负载性能（负载值为3 mol / 1 mol载体）和易于回收的特性，并且液相反应和固体沉淀过程结合了液相肽合成和液相沉淀的优点固相肽合成是一种高产，可扩展，原子经济且环境友好的肽合成方法。该创新方法在有机化学和化学生物学研究领域，尤其是在基于肽的生物医学材料和药物合成领域具有广阔的前景。