作为可多样化的源,非活化烯的区域选择性胺化与迪亚齐林
Qingyu Xing1, Preeti P Chandrachud2, Khalilia Tillett1
1Department of Chemistry, University of South Florida, Tampa, FL, 33620, USA.
这项研究引入了一种新方法,用于合成复杂的化合物,使用迪亚齐林和未激活的烯酸. 这种多功能方法可以有效地制备氨基,氨酸和异循环,包括在天然产品和药品中.
科学领域:
- 有机化学 有机化学
- 合成方法论 合成方法论
- 药用化学 医学化学
背景情况:
- 含的化合物在医学,农业和材料科学中至关重要.
- 合成基化衍生物,特别是在无菌阻碍的环境中,存在重大挑战.
研究的目的:
- 开发一种使用diazirines的多功能和区域选择性方法来胺化未激活的olefins.
- 为了证明这种方法在合成各种含分子中的广泛适用性.
主要方法:
- 不被激活的氨酸的区域选择性胺化与迪亚齐林.
- 在温和的条件下将中间体亚齐里丁转化为初级氨基,氨酸和异环.
- 在保护自然产品的无组胺和制药化合物的合成中应用.
主要成果:
- 报告了50多个成功的氨基化反应的例子.
- 证明了广泛的功能组耐受性,包括酒精,,化物和环氧化物.
- 在五种以目标和多样性为导向的药物化合物合成中成功应用.
- 准备和验证 bis-15N 迪亚齐林用于晚期同位素标签.
结论:
- 开发的方法为复杂的含化合物提供了一条通用的途径.
- 这种方法有助于合成有价值的分子,包括药品和标记化合物.
- 基于Diazirine的水氨基化为有机合成提供了一个强大的工具.
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