Pd(II) - 催化双重循环化 - 化的化
Raju Jannapu Reddy1, Nunavath Sharadha1, Gamidi Rama Krishna2
1Department of Chemistry, University College of Science, Osmania University, Hyderabad 500 007, India.
The Journal of organic chemistry
|June 7, 2023
概括
这项研究引入了一种使用催化剂合成混合硫和醇化合物的新方法. 这些新的乙烯基硫结合分子对制药应用具有前景.
科学领域:
- 有机化学 有机化学
- 药用化学 医学化学
- 催化剂是一种催化剂.
背景情况:
- 甲基和乙烯基硫是关键的制药基因.
- 结合这些支架的混合类型需要进一步调查.
研究的目的:
- 开发一种通用和高效的Pd催化方法,用于合成新型乙烯基硫绑定的硫和醇.
- 探索这些混合支架在药物发现中的潜力.
主要方法:
- -基烯醇/-基烯林与 (E) -β-基烯硫的分子内循环和乙化.
- 在温和条件下进行酸 (Pd(OAc) 2) 催化.
- 以多样性为导向的合成,使C ((sp2) -C ((sp2) 交叉合成为可能.
主要成果:
- 实现了良好的高收益率的乙烯基硫结合的硫和英多尔与优秀的立体选择性.
- 证明了连续过程的可扩展性,直到格拉姆尺度.
- 探索了后期的转化过程,包括异构化和脱硫基-硫化.
结论:
- 开发了一种强大而通用的合成途径,用于新型混合异环化合物.
- 该方法为药物化学和药物发现提供了有价值的工具.
- 提出了可信的反应机制,得到了对照实验的支持.
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