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铜催化兰反应和顺序氧化费舍尔醇合成,以制备醇衍生物
Jia-Yi Gao1, Xian-Jun Wei1, Si-Yu Chen1
1Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources (Ministry of Education of China), Guangxi Key Laboratory of Chemistry and Molecular Engineering of Medicinal Resources, School of Chemistry and Pharmaceutical Sciences, Guangxi Normal University, 15 Yu Cai Road, Guilin 541004, China.
铜催化使α-quinazolin-4-yloxy ketones的高效合成成为可能. 这些化合物是通过单费舍尔醇合成程序合成醇的有价值的前体.
科学领域:
- 有机化学 有机化学
- 合成化学 合成化学
- 催化剂是一种催化剂.
背景情况:
- 基纳索林是一种具有重要意义的异环化合物,具有多样化的生物活性.
- 有效的合成路径到功能化的quinazolinone衍生物对于药物化学至关重要.
- 在药物发现中,Indoles是特权的支架,需要多功能合成方法.
研究的目的:
- 开发一种新型的铜催化方法,用于合成α-quinazolin-4-yloxy ketones.
- 为了探索α-quinazolin-4-yloxy ketones作为醇合成前体的实用性.
- 从α-quinazolin-4-yloxy ketones中建立一个单级联反应,以形成道.
主要方法:
- 铜催化兰合N3-氧基纳和基酸之间的合.
- 随后的[3,3]-重新排列形成α-quinazolin-4-yloxy ketones. 后来的[3,3]-重新排列形成α-quinazolin-4-yloxy ketones. 后来的[3,3]-重新排列形成α-quinazolin-4-yloxy ketones. 后来的[3,3]-重新排列形成α-quinazolin-4-yloxy ketones.
- 费舍尔醇合成,涉及α-quinazolin-4-yloxy ketones与空气中的arylhydrazines的反应.
主要成果:
- 多种α-quinazolin-4-yloxy ketones被合成,产量中等至优异.
- 合成的α-quinazolin-4-yloxy子通过一级联反应有效地转化为英多尔.
- 级联反应显示了广泛的基质范围,良好的功能组耐受性和高的重排选择性.
- 开发的方法提供了对高度标记位置的内醇前体的获取.
结论:
- 已经建立了一种新的,高效的铜催化合成路径,用于α-quinazolin-4-yloxy ketones.
- α-Quinazolin-4-yloxy ketones是通过一级联过程合成醇的多功能前体.
- 这种方法为构建具有药物化学潜在应用的复杂醇衍生物提供了有价值的工具.
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