含天冬氨酸保护肽的制备。克服心衰治疗期间副反应的替代方法。

J Robles, E Pedroso, A Grandas
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引用次数: 0

摘要

用HF/苯甲醚处理肽-树脂Ac-Asn-Ser(Bzl)-Gly-Asp(OFm)-pMeBHA可以切割肽-树脂键并去除苯基,如预期的那样,但也产生杂质(约25%),其中苯基与氟基甲基保护基团连接。所需肽与杂质的分离可以通过反相中压液相色谱法完成。当天冬氨酸的-羧基被2-(4-乙酰-2-硝基苯基)乙基保护时,副反应不会发生。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Preparation of an aspartic acid-containing protected peptide. Alternatives for overcoming a side reaction during HF treatment.

Treatment of the peptide-resin Ac-Asn-Ser(Bzl)-Gly-Asp(OFm)-pMeBHA with HF/anisole cleaves the peptide-resin bond and removes the benzyl group, as expected, but also yields an impurity (ca. 25%) in which the benzyl group is linked to the fluorenylmethyl protecting group. Separation of the desired peptide from the impurity can be accomplished by reversed-phase medium-pressure liquid chromatography. The side reaction does not take place when the gamma-carboxyl of aspartic acid is protected with the 2-(4-acetyl-2-nitrophenyl)ethyl group.

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