Department of Chemistry, Rutgers University, 73 Warren Street, Newark, NJ, 07102, United States.
Chemistry. 2023 Apr 25;29(24):e202300096. doi: 10.1002/chem.202300096. Epub 2023 Mar 20.
Skeletal editing via single-atom insertion reactions involving nitrogen heterocycles have been reported by two innovative and complementary methods for the conversion of pyrroles and indoles to pyridines, quinolines and quinazolines. The use of electrophilic carbonyl cation equivalents and in situ generated nitrenes enables molecular editing to transform heterocycles forming the foundation of best-selling pharmaceuticals. Considering the importance of heterocycles in medicinal chemistry, biology and natural products, these methods offer innovative approach to complex molecular structures by heterocycle diversification and peripheral editing.
通过涉及氮杂环的单原子插入反应进行的骨架编辑，已经报道了两种创新且互补的方法，用于将吡咯和吲哚转化为吡啶、喹啉和喹唑啉。使用亲电羰基阳离子等价物和原位生成的氮宾，使得分子编辑能够转化杂环，形成畅销药物的基础。考虑到杂环在药物化学、生物学和天然产物中的重要性，这些方法通过杂环多样化和外围编辑，为复杂分子结构提供了一种创新的方法。
