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首页> 外文期刊>Bulletin of the Chemical Society of Japan >Ethyl 2-Cyano-2-(hydroxyimino)acetate (Oxyma): An efficient and convenient additive used with tetramethylfluoroformamidinium hexafluorophosphate (TFFH) to replace 1-hydroxybenzotriazole (HOBt) and 1-hydroxy-7-azabenzotriazole (HOAt) during peptide synthesis
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Ethyl 2-Cyano-2-(hydroxyimino)acetate (Oxyma): An efficient and convenient additive used with tetramethylfluoroformamidinium hexafluorophosphate (TFFH) to replace 1-hydroxybenzotriazole (HOBt) and 1-hydroxy-7-azabenzotriazole (HOAt) during peptide synthesis

机译：2-Cyano-2-（hydroxyimino）acetate（Oxyma）：2-Cyano-2-（hydroxyimino）acetate（Oxyma）：一种高效便捷的添加剂，与四甲基氟甲ami六氟磷酸盐（TFFH）一起用于在肽合成过程中替代1-羟基苯并三唑（HOBt）和1-羟基-7-氮杂苯并三唑（HOAt）

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摘要

The appropriateness of ethyl 2-cyano-2-(hydroxyimino)acetate (Oxyma) as a substitute for benzotriazole-based additives, for use in the TFFH approach for peptide synthesis, is discussed in terms of its capacity to control racemization, its coupling efficiency in difficult couplings either for stepwise or segment coupling in solution- and solid-phase coupling. In addition, Boc-based solution-phase peptide synthesis and its stability in the presence of growing peptide chains were studied. Oxyma displayed remarkable results in terms of racemization depression together with impressive coupling efficiency in both solution- and solid-phase synthesis. Furthermore, Oxyma suggests a lower risk of explosion than HOBt and HOAt.
机译：讨论了2-氰基-2-（羟基亚氨基）乙酸乙酯（Oxyma）替代苯并三唑基添加剂用于TFFH肽合成的适用性，从控制外消旋的能力，偶联效率方面进行了讨论。在固相和固相耦合中，可用于逐步或分段耦合的困难耦合。此外，还研究了基于Boc的溶液相肽合成及其在肽链增长的情况下的稳定性。在溶液和固相合成中，Oxyma在消旋消退方面显示出显着的结果，并具有令人印象深刻的偶联效率。此外，Oxyma提示爆炸的危险性低于HOBt和HOAt。

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