走向绿色,可扩展的合成:利用DEG交联聚烯树脂克服疏水性挑战
Othman Al Musaimi1,2, Joshua Tomkins3, Sarah M Barry3
1School of Pharmacy, Newcastle University Newcastle upon Tyne NE1 7RU UK othman.almusaimi@newcastle.ac.uk.
乙烯基醇二甲酸盐 (DEG) -交联聚乙烯 (PS) 树脂增强固相合成 (SPPS) 效率,用于难以实现的. 与DVB-PS树脂相比,DEG-PS树脂的纯度和产量更高,支持绿色化学应用.
科学领域:
- 聚合物化学 聚合物化学
- 有机合成 有机合成
- 生物化学 生物化学
背景情况:
- 传统的双乙 (DVB) -交联聚乙烯 (PS) 树脂在固相合成 (SPPS) 中存在局限性,特别是在复杂的序列中.
- 防水性和减少DVB-PS树脂的灵活性可能会阻碍合成效率并导致副作用.
研究的目的:
- 评估二乙烯糖醇 (DEG) 交联聚乙烯 (PS) 树脂作为用于SPPS的DVB-PS树脂的替代品.
- 评估DEG-PS树脂在合成具有挑战性的的性能及其与绿色化学原则的兼容性.
主要方法:
- 使用DEG-PS和DVB-PS树脂进行的比较合成.
- 对的纯度和产量的分析.
- 对抑制副作用的评估.
- 在合成中应用绿色化学原理.
主要成果:
- 与DVB-PS树脂相比,DEG-PS树脂表现出更好的合成效率,产生更高的纯度和的产量高达28个残留物.
- 特定的挑战性,如ABC模拟物和Thymosin,在DEG-PS树脂上显示出优异的结果.
- DEG-PS树脂有效地抑制了像二形成这样的常见副作用.
- 在绿色化学条件下使用DEG-PS树脂成功合成复杂 (β (34-42),Jung和Redemann (JR) 和ABRF 1992).
结论:
- 对于SPPS,DEG-PS树脂是DVB-PS树脂的优质替代品,为具有挑战性的序列提供了更好的性能.
- 树脂的特性促进了更高的纯度和产量,同时最大限度地减少了副作用.
- DEG-PS树脂支持合成中的绿色化学原理,使其适合工业应用.
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