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Solid-phase Synthesis of [4.4] Spirocyclic Oximes
Published on: February 6, 2019
用黄金催化的一步实用合成来自易于获得的基醇的氧乙-3-
Longwu Ye1, Weimin He, Liming Zhang
1Department of Chemistry and Biochemistry, University of California, Santa Barbara, California 93106, USA.
Journal of the American Chemical Society
|June 5, 2010
概括
一种新的方法在开放式瓶条件下使用基醇合成牛-3-. 这种方法通过黄金碳提供了一条有价值的途径,通过黄金碳来获得oxetan-3-one,这是药物发现的关键中间体.
科学领域:
- 有机化学 有机化学
- 合成化学 合成化学
- 药用化学 医学化学
背景情况:
- 氧得-3-是药物化学中有价值的支架.
- 以前的合成往往涉及危险的试剂或复杂的程序.
研究的目的:
- 开发一种一般的,高效的,安全的oxetan-3-one合成方法.
- 通过使用易于获得的起始材料,建立一种新的氧得-3-one路径.
主要方法:
- 使用醇作为基质.
- 采用黄金催化剂进行分子间基氧化.
- 在环境条件下进行的反应 (开放式瓶).
主要成果:
- 实现了各种氧乙-3-one的一般合成.
- 在一个步骤中从propargyl酒精中制备的oxetan-3-one具有良好的产量.
- 证明了紧张氧乙环的容易形成.
结论:
- 开发的方法提供了一个安全而高效的进入α-oxo金碳化合物的化学.
- 这种方法可以避免使用危险的二基.
- 为药物发现研究提供了有价值的工具.
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