基于循环β-硫的O,S,Se含有Biginelli产品及其后功能化
Kateryna V Dil1,2, Vitalii A Palchykov1
1Research Institute of Chemistry and Geology, Oles Honchar Dnipro National University, Nauky Av. 72, Dnipro, 49045, Ukraine.
Beilstein journal of organic chemistry
|September 3, 2024
概括
一种新的Biginelli合成有效地使用β-硫生产二胺 (DHPMs). 这种方法产生了各种各样的化合物,包括一种潜在的抗癌药物模拟物,具有有前途的生物活性.
科学领域:
- 有机合成 有机合成
- 药用化学 医学化学
- 催化剂是一种催化剂.
背景情况:
- 比吉内利反应是合成二胺基因子 (DHPMs) 的基石.
- 开发DHPM的高效和多功能合成路径对于药物发现至关重要.
- 探索新的催化剂和反应条件可以提高产量和选择性.
研究的目的:
- 为了开发一个单,三组分的Biginelli合成二皮里米丁//selenones.
- 为了研究三酸盐[Yb(OTf) ]作为这种双重反应的催化剂的实用性.
- 合成和评估新的DHPM衍生品,包括含有SO2的enastron类似物.
主要方法:
- 一个,三组分比尼内利反应使用β-硫 (二二H-thiopyran-3(4H) -one-1,1-二氧化物),尿素,和.
- 使用乙酸或无溶剂Yb的催化3.
- 格拉姆尺度合成和随后的Biginelli产品衍生成凝结的提亚和四.
- 在ADMET参数的形评估中.
主要成果:
- 在Biginelli合成中获得的高化学和区域选择性.
- 多种DHPM以高达95%的合理产量进行合成.
- 成功合成了含有SO2的enastron类似物.
- 证明了Biginelli产品的反应性,用于合成冷凝的提亚和四.
- 在中ADMET分析表明大多数化合物具有的相似性.
结论:
- 开发的Biginelli合成为各种DHPM及其衍生品提供了一条有效的途径.
- 该方法适用于潜在的候选药物的克尺度合成.
- 合成的化合物对各种病原体和疾病表现出有希望的生物活性,包括Candida albicans和Leishmania amazonensis.
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