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Two-step, regioselective, multigram-scale synthesis of 2-(trifluoromethyl)indoles from 2-nitrotoluenes
Tetrahedron Letters ( IF 1.5 ) Pub Date : 2021-10-29 , DOI: 10.1016/j.tetlet.2021.153515
Magdalena Walewska-Królikiewicz 1 , Bogdan Wilk 2 , Andrzej Kwast 1 , Zbigniew Wróbel 1
中文翻译：
从 2-硝基甲苯中两步、区域选择性、多克级合成 2-（三氟甲基）吲哚
更新日期：2021-12-03
Tetrahedron Letters ( IF 1.5 ) Pub Date : 2021-10-29 , DOI: 10.1016/j.tetlet.2021.153515
Magdalena Walewska-Królikiewicz 1 , Bogdan Wilk 2 , Andrzej Kwast 1 , Zbigniew Wróbel 1
Affiliation
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The acylation of 2-nitrotoluenes using ethyl trifluoroacetate, one of the least expensive sources of a trifluoromethyl group, produces intermediate 2-nitrobenzyl trifluoromethyl ketones which, without the need for isolation, are cyclized under the action of Zn/AcOH providing 2-(trifluoromethyl)indoles unsubstituted at the C3 position. The developed method avoids the use of expensive catalysts and harsh reaction conditions. The method is readily scalable without a significant decrease in performance upon going from 10- to 250-mmol scale.
中文翻译：
从 2-硝基甲苯中两步、区域选择性、多克级合成 2-（三氟甲基）吲哚
使用三氟乙酸乙酯（三氟甲基的最便宜来源之一）酰化 2-硝基甲苯，产生中间体 2-硝基苄基三氟甲基酮，无需分离，在 Zn/AcOH 的作用下环化，提供 2-（三氟甲基） )在 C3 位置未取代的吲哚。所开发的方法避免了使用昂贵的催化剂和苛刻的反应条件。该方法易于扩展，性能从 10 毫摩尔到 250 毫摩尔不会显着降低。
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