氨基酸通过用化试剂暂时掩盖而形成键
Wataru Muramatsu1, Hisashi Yamamoto1
1Molecular Catalyst Research Center, Chubu University, 1200 Matsumoto-cho, Kasugai, Aichi 487-8501, Japan.
Journal of the American Chemical Society
|April 30, 2021
概括
一种新的单方法使得使用未受保护的氨基酸进行合成. 这种高效的键形成反应避免了种族化和聚合,实现了高产和多功能组耐受性.
科学领域:
- 有机化学
- 类化学
- 合成方法
背景情况:
- 合成传统上需要保护/解除保护的步骤,增加复杂性和成本.
- 开发直接键形成的高效方法对于简化合成至关重要.
研究的目的:
- 通过使用未受保护的氨基酸和来形成单结反应.
- 建立一种高产率且无种族化合成的多功能高效方法.
主要方法:
- 使用两个化试剂,HSi[OCH(CF3) 2 3和MTBSTFA,用于激活和暂时掩盖.
- 使用化 (CsF) 和伊米达作为催化剂,促进化学选择性化.
- 通过直接合未受保护的氨基酸和进行反应.
主要成果:
- 获得高产率,超过99%,没有观察到任何种族化或聚合.
- 已证明对氨基酸侧链具有广泛的功能群耐受性.
- 成功实施了一种单一的键形成策略.
结论:
- 开发的方法为合成提供了高效和多用途的方法.
- 这种单反应通过消除保护组的需要简化了合成.
- 该方法适用于合成具有复杂侧链的.
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