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Solid-phase Synthesis of [4.4] Spirocyclic Oximes
Published on: February 6, 2019
合成石素的异素类型的合成
Yuan Wang1, Zhe Wang1, Miao Zhuang1
1State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Beijing Key Laboratory of Active Substances Discovery and Druggability Evaluation, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China. lxya@imm.ac.cn.
研究人员合成了新型 (±) - 斯特莱丁类同类物与异佐林核心. 关键反应包括Meyer-Schuster重组和复杂结构的氧化循环添加.
科学领域:
- 有机化学 有机化学
- 药用化学 医学化学
背景情况:
- 石素是具有潜在生物活性的天然产品.
- 合成类型的开发对于结构-活性关系研究至关重要.
研究的目的:
- 设计和合成新型 (±) - 隐形蛋白类型.
- 为了探索将一个异佐林环融入到stellettin支架中.
- 建立一种合成路径,用于生成多种类型的类似物.
主要方法:
- 迈耶-舒斯特对关键中间阵型的重新排列.
- 内分子氧化物循环添加用于构建四环性异佐林.
- 维蒂格的反应是为了引入各种侧链.
主要成果:
- 成功合成含有异佐林部分的 (±) - 斯特莱丁类似物.
- 对模拟生成的一种多功能合成策略的演示.
- 合成化合物的表征.
结论:
- 开发的合成途径是有效的生产含有异佐林的丁类同类物.
- 这项工作为进一步探索明星蛋白模拟化学提供了一个平台.
- 合成的类似物可以用于生物评估.
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