Greening Fmoc/tBu solid-phase peptide synthesis,Green Chemistry

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Greening Fmoc/tBu solid-phase peptide synthesis
Green Chemistry ( IF 9.3 ) Pub Date : 2020/01/25 , DOI: 10.1039/c9gc03982a
Othman Al Musaimi _{1,

2,

3,

4,

5} , Beatriz G. de la Torre _{3,

6,

7,

8,

9} , Fernando Albericio _{1,

2,

3,

4,

5}

Affiliation

Peptides are gaining considerable attention as potential drugs. The so-called Fmoc/tBu solid-phase synthesis is the method of choice for the synthesis of these molecules in both research and industrial settings. This synthetic strategy involves a solid polymeric protecting group and allows the use of an excess of reagents to achieve quantitative yields. Intermediates are not isolated. However, extensive washing with solvents is carried out between the synthetic steps. Hazardous solvents, mainly DMF, NMP, and CH₂Cl₂, are currently being used for the chemical reactions and also for the washings. In recent years, several studies have proposed the use of greener solvents in solid-phase peptide synthesis (SPPS). Here we compile all the greening efforts done in this regard and analyze each synthetic step separately. In summary, we can conclude that in many cases green solvents do not impair the synthetic process and that their adoption in current synthetic schemes will be translated into a smaller impact on the environment and on human health.

中文翻译：

绿化Fmoc / tBu固相肽合成

肽作为潜在的药物正受到越来越多的关注。所谓的Fmoc / t Bu固相合成是在研究和工业环境中合成这些分子的选择方法。该合成策略涉及固体聚合物保护基，并允许使用过量的试剂以实现定量收率。中间体不是孤立的。然而，在合成步骤之间用溶剂进行了广泛的洗涤。有害溶剂，主要是DMF，NMP和CH ₂ Cl ₂，目前用于化学反应，也用于洗涤。近年来，一些研究提出在固相肽合成（SPPS）中使用绿色溶剂。在这里，我们汇总了在这方面所做的所有绿化工作，并分别分析了每个合成步骤。总而言之，我们可以得出结论，在许多情况下，绿色溶剂不会损害合成过程，并且在当前的合成方案中采用绿色溶剂将对环境和人类健康产生较小的影响。

更新日期：2020-02-24

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