Synthesis of Biologically Active Heterospirocycles through Iterative 1,3-Dipolar Cycloaddition Pathways.
Synthesis of Biologically Active Heterospirocycles through Iterative 1,3-Dipolar Cycloaddition Pathways.
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通过迭代 1,3-偶极环加成途径合成生物活性杂螺环。
DOI：
10.1021/acs.joc.0c02424
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发表时间：
2021
期刊：
影响因子：
--
通讯作者：
Sharma P
中科院分区：
文献类型：
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作者：
Sharma P
我们首次展示了外亚胺与 1,3-偶极子的新型螺环化，从而产生了螺环中带有仲胺 (NH) 的 3D 螺环。本文描述的合成方法允许获得这些先前未探索的杂螺环核心，其可用于发现医学和材料科学的功能分子。通过发现一类前所未有的对人类原生动物具有抗疟活性的杂螺环化合物，证明了这一点。恶性疟原虫。
We demonstrate the novel spiroannulation ofexo-imines with 1,3-dipoles, for the first time, leading to 3D spirocycles with a secondary amine (NH) in the spiro-ring. The synthetic method described herein allows access to these previously unexplored heterospirocyclic cores that have application in the discovery of functional molecules for medicinal and materials science. This was demonstrated by discovering an unprecedented class of heterospirocycles with antimalarial activity against the human protozoanP. falciparum.