Bayer AG, Innovation Campus Berlin, 13353 Berlin, Germany.
Nuvisan ICB GmbH, 13353 Berlin, Germany.
Molecules. 2021 Mar 22;26(6):1790. doi: 10.3390/molecules26061790.
DNA-encoded libraries (DEL) are increasingly being used to identify new starting points for medicinal chemistry in drug discovery. Herein, we discuss the development of methods that allow the conversion of both primary amines and anilines, attached to DNA, to their corresponding azides in excellent yields. The scope of these diazo-transfer reactions was investigated, and a proof-of-concept has been devised to allow for the synthesis of macrocycles on DNA.
DNA 编码文库 (DEL) 在药物发现中越来越多地被用于鉴定新的药物化学起点。本文讨论了开发方法的进展，这些方法可以将连接在 DNA 上的伯胺和苯胺转化为相应的叠氮化物，产率优异。这些重氮转移反应的范围已经过研究，并设计了一个概念验证，以允许在 DNA 上合成大环。
