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首页> 外文期刊>Chemistry: A European journal >Solid-Phase Synthesis of Peptide Isosters by Nucleophilic Reactions with N-Terminal Peptide Aldehydes on a Polar Support Tailored for Solid-Phase Organic Chemistry
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Solid-Phase Synthesis of Peptide Isosters by Nucleophilic Reactions with N-Terminal Peptide Aldehydes on a Polar Support Tailored for Solid-Phase Organic Chemistry

机译：N-末端肽醛类在固相有机化学专用极性载体上的亲核反应固相合成肽等排体

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摘要

A new concept for the solidphase synthesis of various peptide isosters as potential protease inhibitors is presented. An N-terminal peptide aldehyde was generated on the solid phase by the periodate cleavage reaction. The reactive aldehyde was characterized by MAS NMR on the solid phase and employed as a versatile starting material for various nucleophilic reactions. The reactions conducted include reductive amination, nitroaldol reaction, and the addition of ylides of the Horner-Wadsworth-Emmons type. Furthermore, the addition of silyl-stabilized carbanions and reactions with organometallics of lithium, copper, and zinc were investigated. All solid-phase reactions were carried out on a novel polar resin based on polyethylene glycol tailored for solid-phase organic chemistry. The synthesis and characterization of this resin is presented. Finally, the synthesis of elongated peptide isosters and the preparation of pseudosymmetric peptide isosters is demonstrated.
机译：提出了一种新的概念，用于固相合成各种肽等排体作为潜在的蛋白酶抑制剂。通过高碘酸盐的裂解反应，在固相上生成了N末端肽醛。反应性醛在固相上通过MAS NMR表征，并用作各种亲核反应的通用原料。进行的反应包括还原胺化，硝基醛醇反应和添加霍纳-沃兹沃思-埃蒙斯类型的酰化物。此外，研究了甲硅烷基稳定的碳负离子的添加​​以及与锂，铜和锌的有机金属的反应。所有固相反应均在基于聚乙二醇的新型极性树脂上进行，该极性树脂专为固相有机化学而设计。介绍了该树脂的合成和表征。最后，证明了细长肽等位基因的合成和拟对称肽等位基因的制备。

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