Institute of Chemistry, Saint Petersburg State University, 26 Universitetskii Prospect, Peterhof 198504, Russian Federation.
Org Lett. 2015 Aug 7;17(15):3930-3. doi: 10.1021/acs.orglett.5b02014. Epub 2015 Jul 30.
Significant expansion of heterocyclic product space accessible by the Castagnoli-Cushman reaction (CCR) has been achieved via the use of glutaric anhydride analogues containing endocyclic substitutions with oxygen, nitrogen, and sulfur. Incorporation of these heteroatoms in the anhydride's backbone results in enhanced reactivity and generally lower temperatures that are required for the reactions to go to completion. These findings are particularly significant in light of the CCR recently recognized as an efficient tool for lead-oriented synthesis.
通过使用含有内酰胺取代基的戊二酸酐类似物，包括氧、氮和硫，已经实现了通过 Castagnoli-Cushman 反应（CCR）可获得的杂环产物空间的显著扩展。在酐的主链中引入这些杂原子会导致反应性增强，通常所需的反应温度也会降低，从而使反应完全进行。鉴于 CCR 最近被认为是一种用于导向合成的有效工具，这些发现尤其重要。
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