Mixing of polystyrene resins in solid-phase synthesis is performed by shaking or gentle agitation of the reaction vessel to avoid breaking the brittle beads. These mixing strategies result in poor diffusion to and into the beads. Using a large excess of reagents is the common way to compensate for these deficiencies. We use fast overhead stirring for performing coupling reactions on a solid support. We show that fast overhead stirring enhances the efficiency of amide bond formation on the solid support compared to the state-of-the-art mixing method, while preserving the integrity of the beads. We find that fast overhead stirring minimizes the effect of decomposition of the activated species by increasing the diffusion-dependent coupling reaction. This allows decreasing the excess of reagents used for the multistep synthesis of peptides, thus providing a greener and more sustainable alternative for peptide synthesis on solid supports.

中文翻译：

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固体载体上的扩散增强型酰胺键形成

通过摇动或轻轻搅拌反应容器来进行固相合成中的聚苯乙烯树脂的混合，以避免使脆性珠粒破裂。这些混合策略导致向和向珠的扩散不良。使用大量过量的试剂是弥补这些缺陷的常用方法。我们使用快速的塔顶搅拌在固体载体上进行偶联反应。我们显示，与现有技术的混合方法相比，快速的塔顶搅拌提高了固相支持物上酰胺键形成的效率，同时保留了珠粒的完整性。我们发现快速的塔顶搅拌通过增加扩散依赖性偶联反应使活化物质分解的影响最小化。这样可以减少用于肽的多步合成的试剂过量，