期刊
ADVANCED SYNTHESIS & CATALYSIS
卷 364, 期 10, 页码 1724-1731出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/adsc.202101451
关键词
photochemistry; radical reactions; annulation; heterocycles; synthetic methods
资金
- EPSRC Centre for Doctoral Training in Synthesis for Biology and Medicine [EP/L015838/1]
- AstraZeneca
- Diamond Light Source
- Defence Science and Technology Laboratory
- Evotec
- GlaxoSmithKline
- Janssen
- Novartis
- Pfizer
- Syngenta
- Takeda
- UCB
- Vertex
- St John's College Oxford
In this study, a metal-free, visible light-mediated cyclization of malonates onto 5-ring heteroaromatics is reported. The method eliminates the need for transition metals or toxic tin reagents and instead utilizes iodomalonates as key intermediates. The annulated products are obtained in good yields (46-94%) without the use of external catalysts.
Annulated heteroaromatics can be accessed through the addition of malonyl radicals onto heterocycles. Current methods are applicable to electron-rich heteroaromatics and reliant on transition metals or toxic tin reagents. Here we report a metal-free, visible light-mediated cyclisation of malonates onto 5-ring heteroaromatics using iodomalonates as key intermediates. The iodomalonates are prepared and photolysed in situ to give the desired annulated products, in yields of 46-94% without the need for external catalysts. The scope of this transformation includes N-alkyl, N-acyl and carbon-tethered malonates adding onto a wide range of 5-membered heteroaromatics.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据