Complexation of Polyethyleneglycol Containing Small Molecules with Magnesium Chloride as a Purification and Isolation Strategy,Organic Process Research & Development

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Complexation of Polyethyleneglycol Containing Small Molecules with Magnesium Chloride as a Purification and Isolation Strategy
Organic Process Research & Development ( IF 3.1 ) Pub Date : 2021-09-10 , DOI: 10.1021/acs.oprd.1c00174
Bin Zheng ₁ , Jun Li ₁ , Charles Pathirana ₁ , Shenjie Qiu ₁ , Michael A. Schmidt ₁ , Martin D. Eastgate ₁

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Polyethyleneglycol (PEG) containing compounds are often non-crystalline, gel-like oils, which pose great challenges for handling, purification, and isolation, particularly on large scales. To overcome these isolation challenges, a new procedure has been established, which is based on the discovery that complexation with magnesium chloride (MgCl₂) can transform these oily intermediates into solid complexes. This method significantly improves the handling of PEG compounds and leads a more process-friendly isolation for larger scale handling. Often, the resulting PEG–MgCl₂ complexes could be used directly in subsequent transformations, such as a peptide coupling. Alternately, the inorganic Mg salt used in these weakly bonded complexes can be readily dissociated and removed from the desired PEG derivatives.

中文翻译：

含小分子聚乙二醇与氯化镁络合作为纯化和分离策略

含有聚乙二醇 (PEG) 的化合物通常是非结晶的、凝胶状的油，这对处理、纯化和分离提出了巨大的挑战，尤其是在大规模的情况下。为了克服这些分离挑战，已经建立了一种新程序，该程序基于与氯化镁 (MgCl ₂ )络合可以将这些油性中间体转化为固体复合物的发现。这种方法显着改善了 PEG 化合物的处理，并为更大规模的处理带来了对工艺更友好的分离。通常，由此产生的 PEG-MgCl ₂复合物可直接用于后续转化，例如肽偶联。或者，在这些弱键合复合物中使用的无机镁盐可以很容易地从所需的 PEG 衍生物中解离和去除。

更新日期：2021-10-15

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