Khan Shahnawaz, Ansari Monish Arbaz, Singh Maya Shankar
Department of Chemistry, Institute of Science, Banaras Hindu University, Varanasi, Uttar Pradesh221005, India.
Org Lett. 2023 Feb 3;25(4):642-646. doi: 10.1021/acs.orglett.2c04223. Epub 2023 Jan 19.
We describe herein a chemo- and regioselective cascade annulation between β-ketothioamides and diazo-substituted hypervalent iodine reagents under transition-metal-free and base-free conditions at room temperature. Thus, a divergent construction of fused-heterocyclic scaffold thiazolothiadiazoles has been achieved with the advantages of operational simplicity, scalability, broad substrate compatibility, and mild reaction conditions. This one-pot strategy not only avoids potential toxicity but also broadens the arsenal of synthetic methods to obtain fused ,-heterocyclic frameworks.
我们在此描述了一种在室温下无过渡金属和无碱条件下，β-酮硫代酰胺与重氮取代的高价碘试剂之间的化学选择性和区域选择性串联环化反应。因此，实现了稠合杂环骨架噻唑并噻二唑的多样化构建，具有操作简单、可扩展性强、底物兼容性广和反应条件温和等优点。这种一锅法策略不仅避免了潜在的毒性，还拓宽了获得稠合杂环骨架的合成方法库。
