改进伪脯氨酸和 DMB 二肽羧酸的合成

Synlett Pub Date : 2024-04-15 DOI:10.1055/a-2306-9316

Wyatt C. Powell, Kelly Johnson, Peyton Tran, Ruiheng Jing, Maciej Walczak

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引用次数: 0

摘要

我们报告了一种温和的方法，用于制备含有 DMB (HMB) 基团或修饰为假脯氨酸的 Fmoc 保护二肽。为了尽量减少 Fmoc 保护的损失，我们优化了皂化条件，并加入了一种钙添加剂，以保护其他碱敏感官能团并提高游离酸的产率（36-82%）。反应需要在室温下在 i-PrOH 和水的混合物中加入 CaCl2 和 NaOH。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

Improved Synthesis of Pseudoproline and DMB Dipeptide Carboxylic Acids

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Improved Synthesis of Pseudoproline and DMB Dipeptide Carboxylic Acids

We report a mild method for the preparation of Fmoc-protected dipeptides containing a DMB (HMB) group or modified as pseudoprolines. To minimize the loss of the Fmoc protection, we optimized the saponification conditions and included a calcium additive that protected the other base-sensitive functionalities and improved the yield of the free acid (36-82%). The reaction requires a combination of CaCl2 and NaOH in a mixture of i-PrOH and water at room temperature.

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Synlett

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