2-Ethylquinazolin-4-one derivatives bearing various ortho-substituted phenyl groups were revealed to possess a stable C–N axially chiral structure at ambient temperature. The reactions of alkyl halides with the anionic species prepared from these quinazolinones were systematically explored. The α-alkylation reactions proceeded with diastereoselectivities ranging from 1:1 to >50:1, depending upon the steric bulk of the ortho-substituent, to afford products having the elements of axial and central chirality in high yields (85–98%).

中文翻译：

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带有各种邻位取代苯基的 N-C 轴向手性喹唑啉酮衍生物的 α-烷基化：非对映选择性与邻位取代基的关系

带有各种邻位取代苯基的 2-Ethylquinazolin-4-one 衍生物被证明在环境温度下具有稳定的 C-N 轴向手性结构。系统地研究了卤代烷与由这些喹唑啉酮制备的阴离子物质的反应。α-烷基化反应以 1:1 到 >50:1 的非对映选择性进行，这取决于邻位取代基的空间体积，以高产率（85-98%）提供具有轴和中心手性元素的产物.