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首页> 外文期刊>Chemistry: A European journal >Oxyma: An Efficient Additive for Peptide Synthesis to Replace theBenzotriazole-Based HOBt and HOAt with a Lower Risk of Explosion~[1]
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Oxyma: An Efficient Additive for Peptide Synthesis to Replace theBenzotriazole-Based HOBt and HOAt with a Lower Risk of Explosion~[1]

机译：Oxyma：一种肽合成的有效添加剂，可取代具有爆炸危险的苯并三唑基HOBt和HOAt，[1]

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摘要

Oxyma [ethyl 2-cyano-2-(hy-droxyimino)acetate] has been tested asan additive for use in the carbodiimideapproach for formation of peptidebonds. Its performance in relation tothose of HOBt and HOAt, which haverecently been reported to exhibit ex-plosive properties, is reported. Oxymadisplayed a remarkable capacity to in-hibit racemization, together with im-pressive coupling efficiency in both au-tomated and manual synthesis, superiorto those of HOBt and at least compa-rable to those of HOAt, and surpassingthe latter coupling agent in the more demanding peptide models. Stabilityassays showed that there was no risk ofcapping the resin under standard cou-pling conditions. Finally, calorimetryassays (DSC and ARC) showed de-composition profiles for benzotriazole-based additives that were consistentwith their reported explosivities andsuggested a lower risk of explosion inthe case of Oxyma.
机译：氧[2-氰基-2-（羟基亚氨基亚氨基）乙酸乙酯]已被测试用作碳二亚胺方法中形成肽键的添加剂。据报道其相对于HOBt和HOAt的性能，最近已经报道其表现出爆炸性。 Oxyma具有出色的抑制外消旋能力，在自动和手动合成中均表现出令人印象深刻的偶联效率，优于HOBt，至少可与HOAt相比，并且在要求更高的方面超过了后者肽模型。稳定性分析表明，在标准偶联条件下没有封端树脂的风险。最后，量热分析（DSC和ARC）显示出基于苯并三唑的添加剂的分解曲线，与所报道的爆炸性相符，在氧气不足的情况下，爆炸的风险较低。

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