Dearomatization reactions allow the direct synthesis of structurally complex sp³-rich molecules from readily available “flat” precursors. Established dearomatization processes commonly involve the formation of new C−C bonds, whereas methods that enable the introduction of C−N bonds have received less attention. Because of the privileged position of nitrogen in drug discovery, significant recent methodological efforts have been directed towards addressing this deficiency. Consequently, a variety of new processes are now available that allow the direct preparation of sp³-rich amino-containing building blocks and scaffolds. This review gives an overview of C−N bond forming dearomatization reactions, particularly with respect to scaffold assembly processes. The discussion gives historical context, but the main focus is on selected methods that have been reported recently.

中文翻译：

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脱芳胺化反应

脱芳构化反应允许从容易获得的“扁平”前体直接合成结构复杂的富含sp ^{3 的}分子。已建立的脱芳构化过程通常涉及形成新的 C-C 键，而能够引入 C-N 键的方法受到的关注较少。由于氮在药物发现中的特权地位，最近的重大方法学努力已针对解决这一缺陷。因此，现在有多种新工艺可以直接制备 sp ³- 富含氨基的积木和支架。本综述概述了 CN 键形成脱芳构化反应，特别是支架组装过程。讨论给出了历史背景，但主要关注最近报道的选定方法。