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Solid-phase Synthesis of [4.4] Spirocyclic Oximes
Published on: February 6, 2019
通过将氧化物循环转化为和双极循环添加,制备螺旋环氧化物
Beth L Ritchie1, Alexandra Longcake2, Iain Coldham1
1Chemistry, School of Mathematical and Physical Sciences, University of Sheffield, Sheffield S3 7HF, UK.
研究人员使用一种新的子循环添加合成了复杂的螺旋氧indoles. 这种高效的级联反应为潜在的药物发现创造了有价值的化合物.
科学领域:
- 有机化学 有机化学
- 药用化学 医学化学
- 化学合成 化学合成
背景情况:
- 氧醇是药物化学中的关键支架,表现出多样化的生物活动.
- 螺旋环框架在许多天然产品和药理活性分子中普遍存在.
研究的目的:
- 开发一种高效的合成策略,用于构建螺旋氧.
- 探索分子间子循环添加对于螺旋循环形成的有用性.
主要方法:
- 通过从化物中通过氧化物循环生成一个二极体的现场生成.
- 分子间子循环添加反应形成螺旋氧.
- 使用单晶X射线衍射和封装纳米滴体结晶 (ENaCt) 的立体化学分析.
主要成果:
- 一个涉及凝结,循环化和循环添加的级联反应被成功运用.
- 复杂的螺旋氧indole产品迅速合成高效率.
- 通过X射线结晶学阐明了关键的螺旋氧醇中间体的立体化学.
结论:
- 开发的子循环添加提供了一种强大的方法来合成复杂的螺旋氧化.
- 这种方法提供了新的oxindole衍生品,在药物发现中具有潜在的应用.
- 级联策略可以快速构建复杂的分子架构.
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