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铜催化(杂)芳基硼酸频哪醇酯与叶立德氟化物的三氟甲基化反应

Copper-Catalyzed Trifluoromethylation of (Hetero)aryl Boronic Acid Pinacol Esters with YlideFluor.

作者信息

Liu Jing, Xiao Yisa, Hao Jian, Shen Qilong

机构信息

Department of Chemistry, Shanghai University, 99 Shangda Road, Shanghai 200444, P. R. China.

Key Laboratory of Organofluorine Chemistry, Shanghai Institute of Organic Chemistry, University of Chinese Academy of Sciences, Chinese Academy of Sciences, 345 Lingling Lu, Shanghai 200032, P. R. China.

出版信息

Org Lett. 2023 Feb 24;25(7):1204-1208. doi: 10.1021/acs.orglett.3c00206. Epub 2023 Feb 13.

Abstract

A copper-catalyzed trifluoromethylation of (hetero)arylboronic acid pinacol esters with YlideFluor for the preparation of trifluoromethylated (hetero)arenes was described. The reaction conditions are mild and compatible with a broad range of functional groups. Heteroaryl boronic acid pinacol esters could also be trifluoromethylated in high yields. Application of this protocol for trifluoromethylation of drug and OLED molecules was demonstrated.

摘要

描述了一种用叶立德氟化物通过铜催化(杂)芳基硼酸频哪醇酯的三氟甲基化反应来制备三氟甲基化(杂)芳烃的方法。该反应条件温和,与多种官能团兼容。杂芳基硼酸频哪醇酯也能以高产率进行三氟甲基化反应。展示了该方法在药物和OLED分子三氟甲基化反应中的应用。

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