Concise Synthesis of Versatile Imidazo[5,1-f][1,2,4]triazin-4(3H)-ones,Organic Process Research & Development

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Concise Synthesis of Versatile Imidazo[5,1-f][1,2,4]triazin-4(3H)-ones
Organic Process Research & Development ( IF 3.1 ) Pub Date : 2018-01-11 00:00:00 , DOI: 10.1021/acs.oprd.7b00333
Tuan P. Tran ₁ , Ethan L. Fisher ₁ , Ann S. Wright ₁ , Jiao Yang ₂

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The synthesis of a series of imidazo[5,1-f][1,2,4]triazin-4(3H)-ones was developed from starting imidazoles in three linear steps. The synthetic sequence began with an electrophilic amination and thus a rigorous campaign to identify safe reagent and reaction conditions was performed to ensure safety for preparation of these versatile intermediates on large scales. Functionalizations at the key positions on these substrates were exemplified to demonstrate ability to perform late-stage diversification for efficient SAR discovery.

中文翻译：

多功能咪唑并[5,1- f ] [1,2,4]三嗪-4（3 H）-ones的简捷合成

从三步线性咪唑起始物，开发了一系列咪唑并[5,1- f ] [1,2,4]三嗪-4（3 H）-ones的合成。合成过程始于亲电胺化反应，因此进行了严格的鉴定安全试剂和反应条件的活动，以确保大规模制备这些通用中间体的安全性。以这些底物上关键位置的功能化为例，以展示执行后期多样化以进行有效SAR发现的能力。

更新日期：2018-01-11

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