Asymmetric construction of densely functionalized three-dimensional aza-tetracyclic scaffolds for drug discovery
Asymmetric construction of densely functionalized three-dimensional aza-tetracyclic scaffolds for drug discovery
复制标题
用于药物发现的密集功能化三维氮杂四环支架的不对称构建
DOI：
10.1039/d2cc05700j
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发表时间：
2022
影响因子：
4.9
通讯作者：
Nakamura Hiroyuki
中科院分区：
文献类型：
--
作者：
Umedera Kohei;Morita Taiki;Nakamura Hiroyuki
通过分子内Diels-Alder反应，由L-酪氨酸衍生的双环前体实现了密集功能化的三维氮杂四环支架的不对称构建。三种取代基以各种组合系统地引入到所开发的支架中，证明了它们在药物发现中的高实用性。
Asymmetric construction of densely functionalized three-dimensional aza-tetracyclic scaffolds were achieved by intramolecular Diels–Alder reaction of bicyclic precursors derived from L-tyrosine. Three substituents were systematically introduced into the developed scaffolds in various combinations, demonstrating their high utility in drug discovery.