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Synthesis of a Series of Diaminoindoles
The Journal of Organic Chemistry ( IF 3.6 ) Pub Date : 2021-08-05 , DOI: 10.1021/acs.joc.1c00652
James S Martin 1 , Claire J Mackenzie 1 , Ian H Gilbert 1
Affiliation  

A selection of 3,4-diaminoindoles were required for a recent drug discovery project. To this end, a 10-step synthesis was developed from 4-nitroindole. This synthesis was subsequently adapted and used to synthesize 3,5-; 3,6-; and 3,7-diaminoindoles from the corresponding 5-, 6-, or 7-nitroindole. These novel intermediates feature orthogonal protecting groups that allow them to be further diversified. This is the first reported synthesis of these types of compounds.

中文翻译:

一系列二氨基吲哚的合成

最近的一个药物发现项目需要选择 3,4-二氨基吲哚。为此,从 4-硝基吲哚开发了 10 步合成。该合成随后被改编并用于合成 3,5-; 3,6-; 和来自相应的 5-、6-或 7-硝基吲哚的 3,7-二氨基吲哚。这些新型中间体具有正交保护基团,使它们能够进一步多样化。这是首次报道的这类化合物的合成。
更新日期:2021-09-03
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