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Decarboxylative cross-couplings of 2-aminopyrimidine-5-carboxylic acids
Tetrahedron ( IF 2.1 ) Pub Date : 2018-05-18 , DOI: 10.1016/j.tet.2018.05.018
Ngoc Son Le Pham , Jihong Lee , Hyunik Shin , Jeong-Hun Sohn

Decarboxylative CC cross-couplings of 2-aminopyrimidine-5-carboxylic acids under a Pd/Ag-based catalytic system opens a new platform for the introduction of diverse C5 substituents. The reaction methods proceeded efficiently with a wide range of the acids and the coupling partners of aryl iodides, alkenes, bromoalkynes, and azoles. Considering ready availability of 2-aminopyrimidine-5-carboxylic acid from the oxidative dehydrosulfurative CN cross-coupling of the 3,4-dihydropyrimidin-1H-2-thiones, this reaction method unambiguously pave a shortcut to densely substituted 2-aminopyrimidine derivatives with unprecedented diversity.



中文翻译:

2-氨基嘧啶-5-羧酸的脱羧交叉偶联

在基于Pd / Ag的催化体系下2-氨基嘧啶-5-羧酸的脱羧C C交叉偶联为引入各种C 5取代基提供了一个新平台。该反应方法使用多种酸和芳基碘化物,烯烃,溴炔烃和唑类的偶合剂有效地进行了反应。考虑到3,4-二氢嘧啶-1 H -2-硫酮的氧化脱氢C N交叉偶联可轻松获得2-氨基嘧啶-5-羧酸,该反应方法无疑为密集取代的2-氨基嘧啶衍生物铺平了捷径。具有前所未有的多样性。

更新日期:2018-05-18
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