First Steps for the Direct Purification of l-Leu-l-Leu Dipeptide through Co-Crystallization,Crystal Growth & Design

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First Steps for the Direct Purification of l-Leu-l-Leu Dipeptide through Co-Crystallization
Crystal Growth & Design ( IF 3.2 ) Pub Date : 2018-01-03 00:00:00 , DOI: 10.1021/acs.cgd.7b01516
Paolo Lucaioli ₁ , Elisa Nauha ₁ , Ishwar Singh ₁ , Nicholas Blagden ₁

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Trifluoroacetate salt contamination of peptides represents a challenging issue related to solid phase peptide synthesis and purification because it affects the chemical and biological properties of peptides. Purification of such materials is typically performed through a two-step post-synthetic procedure based on chromatography followed by ion exchange. For the first time, co-crystallization is presented in this study as a possible alternative and advantageous single-step method for the obtaining of TFA-free crystals of a dipeptide. A trifluoroacetate-contaminated l-Leu-l-Leu dipeptide has been used for co-crystallization experiments along with different solid coformers. New multicomponent crystals containing only the title compound and the second co-crystal formers are described in this work. Such results represent a novelty in the field of peptide chemistry and a valid proof for the use of crystal engineering-based method for a combined purification and crystallization strategy.

中文翻译：

通过共结晶直接纯化l-Leu-Leu-Leu二肽的第一步

肽的三氟乙酸盐污染代表了与固相肽合成和纯化有关的具有挑战性的问题，因为它会影响肽的化学和生物学特性。此类材料的纯化通常通过基于色谱的两步后合成程序进行，然后进行离子交换。首次在本研究中提出共结晶法，作为获得二肽无TFA晶体的一种可能的替代方法和有利的单步方法。三氟乙酸污染的升-Leu-升-Leu二肽已与不同的固体共形成剂一起用于共结晶实验。在这项工作中描述了仅包含标题化合物和第二种共晶形成剂的新的多组分晶体。这样的结果代表了肽化学领域的新颖性，是使用基于晶体工程的方法进行组合纯化和结晶策略的有效证据。

更新日期：2018-01-03

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