维洛西明及其衍生物的简要合成
Barbara Chatinovska1, Rokas Gegevičius1, Edvinas Orentas1
1Department of Organic Chemistry, Institute of Chemistry, Vilnius University, Naugarduko 24, LT-03225 Vilnius, Lithuania.
The Journal of organic chemistry
|June 2, 2023
概括
这项研究提出了使用C2-对称前体的维洛西明反体的高效合成. 这种新的策略允许快速访问和多样化这一重要的化物支架.
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:
- 维洛西明及其衍生物是具有显著生物活性的类化合物.
- 现有的合成途径可能很长,缺乏酶选择性.
- 对于药理学研究来说,获得质纯的化物至关重要.
研究的目的:
- 开发一个快速和enantioselective合成的vellosimine及其衍生品.
- 建立一个多功能策略,以使维洛西米尼支架多样化.
- 为了利用一个负担得起且易于获得的性前体.
主要方法:
- 一个C2-对称的9-azabicyclo[3.3.1]nonane前体的脱对称.
- 内部分子循环形成一个关键的中间体与差异化碳基组.
- 维洛西明组合的晚期地点选择性内化.
主要成果:
- 成功合成了维洛胺的两个反体.
- 证明了化物支架的直接多样化.
- 建立了一个简洁而高效的合成路线.
结论:
- 报告的策略提供了快速获取对异构纯的维洛西明的机会.
- 这种方法可以轻松实现多样化,为新药发现开辟了道路.
- 使用一个负担得起的性前体增强了合成的实用性.
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