Peptide synthesis: ball-milling, in solution, or on solid support, what is the best strategy?

被引：50

作者：

Maurin, Ophelie ^{[1
]}

Verdie, Pascal ^{[1
]}

Subra, Gilles ^{[1
]}

Lamaty, Frederic ^{[1
]}

Martinez, Jean ^{[1
]}

Metro, Thomas-Xavier ^{[1
]}

机构：

[1] Univ Montpellier, ENSCM, CNRS, IBMM,UMR 5247, Campus Triolet,Cc1703,Pl Eugene Bataillon, F-34095 Montpellier 5, France

来源：

BEILSTEIN JOURNAL OF ORGANIC CHEMISTRY | 2017年 / 13卷

关键词：

ball-mill; green chemistry; mechanochemistry; peptide synthesis; SPPS; GREEN CHEMISTRY; AMINO-ACIDS; AMIDE; MECHANOSYNTHESIS; THERAPEUTICS; DIPEPTIDES; SOLVENTS;

D O I：

10.3762/bjoc.13.206

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

While presenting particularly interesting advantages, peptide synthesis by ball-milling was never compared to the two traditional strategies, namely peptide syntheses in solution and on solid support (solid-phase peptide synthesis, SPPS). In this study, the challenging VVIA tetrapeptide was synthesized by ball-milling, in solution, and on solid support. The three strategies were then compared in terms of yield, purity, reaction time and environmental impact. The results obtained enabled to draw some strengths and weaknesses of each strategy, and to foresee what will have to be implemented to build more efficient and sustainable peptide syntheses in the near future.

引用

页码：2087 / 2093

页数：7

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