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CuI/I2‐Mediated Intramolecular Oxidative Cyclization Reaction of N‐(2‐pyridyl)amidines by the Direct Double C−H Functionalization of a C(sp3)−H Bond
Asian Journal of Organic Chemistry ( IF 2.8 ) Pub Date : 2017-10-12 , DOI: 10.1002/ajoc.201700442
Fengping Yi 1 , Songxing Zhang 1 , Lirong Zhang 1 , Weiyin Yi 1 , Rui Yu 2
Affiliation  

A facile approach to a rare class of 3,3‐disubstituted 2‐iminoimidazo[1,2‐a]‐pyridines bearing a hydroxyl group at the 3 position in good to excellent yields from N‐(2‐pyridyl)amidines substrates in the presence of CuI/I2/KI/KOtBu is described. According to the investigation, the use of a Cu catalyst and the presence of sulfonyl groups in the substrates has a remarkable influence on the success of the oxidative cyclization reaction. Moreover, the oxygen source of the hydroxyl group may be from the incorporation of water in the reaction system or KOtBu. The successful implementation of the reaction further indicates that amidines have abundant reactivity under various reaction conditions. The methodology is operationally simple and has a broad substrate scope.

中文翻译:

N-(2-吡啶基)H的CuI / I2-介导的分子内氧化环化反应通过C(sp3)-H键的直接双C-H官能化

一种简便的方法来罕见的类的3,3-二取代-2- iminoimidazo [1,2] -pyridines在良好3位以优异的产率从轴承羟基ñ - (2-吡啶基)脒在基板描述了CuI / I 2 / KI / KO t Bu的存在。根据研究,在基材中使用铜催化剂和磺酰基的存在对氧化环化反应的成功有显着影响。而且,羟基的氧源可以来自在反应体系中的水或KO t的引入。卜 反应的成功实施进一步表明am在各种反应条件下具有丰富的反应性。该方法操作简单,具有广泛的底物范围。
更新日期:2017-10-12
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