来自Pd催化1,5-二-1,2,3-三醇的取消的五环芳香 heterocycles
Kaylen D Lathrum1, Emily M Hanneken1, Katelyn R Grzelak1
1Department of Chemistry and Biochemistry, Creighton University, 2500 California Avenue, Omaha, NE 68178, USA.
研究人员使用催化废除合成了新型五环芳香异环环. 这些化合物,包括功能化氨酸,对细菌和酵母菌具有显著的抗微生物活性.
科学领域:
- 有机化学 有机化学
- 药用化学 医学化学
- 异环化学 异环化学
背景情况:
- 五环芳香异环环在药物化学中是关键的支架.
- 开发高效的合成路径,以功能化氨酸,氨酸和氨酸仍然是一个活跃的研究领域.
- 催化无效提供了一个强大的方法来构建复杂的芳香系统.
研究的目的:
- 通过Pd催化取消1,5-二-1,2,3-三醇合成新型五环芳香异环.
- 在不同的反应条件下,研究替代物连接 (N1与C1) 对不同反应条件下的废除效率的影响.
- 为了评估合成化合物的抗菌性质.
主要方法:
- 合成1,5-二-1,2,3-三醇与 орто-基子单元.
- 在微波辐射和常规热加热下发生的催化无效反应.
- 使用NMR光谱学和UV可见光谱学进行表征.
- 使用最小抑制度 (MIC) 测定进行抗菌活性评估.
主要成果:
- 成功合成功能化的氨酸,纳氨酸和氨酸.
- 在微波辐射下,N1连接的类似物产生了31-90%的产品.
- 连接到C1的类似产品需要热加热,产品的产量在31-65%之间.
- 与未取消的前体相比,取消的化合物表现出红移紫外线可见光谱和增强的光.
- 五种二二四林区域异构体显示出显著的抗菌活性 (MIC 2-16μM).
结论:
- Pd催化无效化是合成五环芳香 heterocycles 的有效策略.
- 反应条件和替代剂连接性显著影响取消结果.
- 合成的二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二二
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