A tertiary amine-mediated highly regioselective aromatic nucleophilic substitution (S_NAr) protocol was developed in the assemblies of perfluorinated phtalimide with primary or secondary amines as inputs. Application of 1-methyl-4-hydroxypiperidine as additive, formation of the less favoured, bioactive regioisomer was facilitated, modifying their ratios from the initial 8–36% to 81–91%. After optimization, a facile gram scale syntheses were accomplished and isolated the desired analogues in up to 63% yield.

中文翻译：

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全氟邻苯二甲酰亚胺核心上的高度区域选择性的4-羟基-1-甲基哌啶介导的芳香亲核取代

在以伯胺或仲胺为输入的全氟化邻苯二甲酰亚胺的组装物中，开发了叔胺介导的高度区域选择性芳族亲核取代（S _N Ar）方案。1-甲基-4-羟基哌啶作为添加剂的应用，促进了较不受欢迎的生物活性区域异构体的形成，将其比例从最初的8–36％更改为81–91％。优化后，完成了简便的克级合成，并以高达63％的收率分离了所需的类似物。