Palladium-Catalyzed Base-Promoted Arylation of Unactivated C(sp3 )-H Bonds by Aryl Iodides: A Practical Approach To Synthesize β-Aryl Carboxylic Acid Derivatives,European Journal of Organic Chemistry

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Palladium-Catalyzed Base-Promoted Arylation of Unactivated C(sp3 )-H Bonds by Aryl Iodides: A Practical Approach To Synthesize β-Aryl Carboxylic Acid Derivatives
European Journal of Organic Chemistry ( IF 2.5 ) Pub Date : 2017-11-15 , DOI: 10.1002/ejoc.201701215
Quan Gou ₁ , Gang Liu ₁ , Lanxiu Zhou ₁ , Suiyun Chen ₂ , Jun Qin ₁

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A highly efficient protocol for the β-arylation of carboxylic amides by aryl iodides under PdCl2(CH3CN)2/CsOAc catalysis was developed. This method was found to tolerate a broad scope of substrates and was successfully employed in the preparation of a variety of β-aryl α-amino and γ-amino acid derivatives. The utility of this method was further illustrated in the synthesis of the psychotropic drug (±)-phenibut and β-aryl bile acid analogues.

中文翻译：

钯催化碱促进芳基碘对未活化 C(sp3)-H 键的芳基化：合成 β-芳基羧酸衍生物的实用方法

开发了一种高效的方案，用于在 PdCl2(CH3CN)2/CsOAc 催化下芳基碘化物对羧酰胺进行 β-芳基化。发现该方法可耐受广泛的底物，并成功用于制备各种 β-芳基 α-氨基和 γ-氨基酸衍生物。这种方法的效用在精神药物 (±)-phenibut 和 β-芳基胆汁酸类似物的合成中得到了进一步说明。

更新日期：2017-11-15

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