从素β-O-4片段合成伊米达佐[1,2-a]皮里丁衍生物,通过单多元组分反应
Luxian Guo1,2, Yangming Ding1, Hua Wang1
1CAS Key Laboratory of Science and Technology on Applied Catalysis, Dalian Institute of Chemical Physics, Chinese Academy of Sciences, Dalian 116023, China.
iScience
|May 30, 2023
概括
这项研究提出了一种单一的方法,将红素转化为有价值的含N的化学物质. 该过程有效地从素衍生物中合成imidazo[1,2-a]pyridines,这些是重要的制药构建块.
科学领域:
- 生物炼油厂和可持续化学
- 有机合成和催化剂.
- 药用化学 医学化学
背景情况:
- 红素的价值化是可持续生物炼油厂的关键.
- 对药品而言,有效合成含N的异环环非常重要.
- 现有的素转化方法往往缺乏效率或多功能性.
研究的目的:
- 开发一种新的单一策略,用于将红素衍生物转化为N-异环化合物.
- 为了探索从素β-O-4模型化合物中合成的imidazo[1,2-a]pyridines.
- 为了证明这种方法在药物合成中的应用.
主要方法:
- 设计了一个单催化转化策略.
- 作为基板,使用了宁β-O-4模型化合物和一种聚合物.
- 2-阿米诺皮里丁作为的来源.
主要成果:
- 获得了高产量 (高达95%) 的imidazo[1,2-a]pyridines.
- 这种转换涉及C-O键裂变,C-H激活和脱水合.
- 合成了各种各样的功能化的imidazo[1,2-a]pyridines.
结论:
- 开发的协议使得从素中有效合成有价值的N-异环化合物.
- 合成的化合物与已知的制药剂具有结构上的相似性.
- 这突显了素衍生物在药物发现和合成中的潜力.
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