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利用氨基酸作为导向基团,镍(II)催化未活化芳基C-H键的单选择性芳基化反应。

Ni(ii)-catalyzed mono-selective -arylation of unactivated aryl C-H bonds utilizing amino acids as a directing group.

作者信息

Cong Zhanqing, Gao Feng, Liu Hong

机构信息

State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences 555 Zu Chong Zhi Road Shanghai 201203 China

University of Chinese Academy of Sciences No. 19A Yuquan Road Beijing 100049 China.

出版信息

RSC Adv. 2019 Apr 8;9(19):10820-10824. doi: 10.1039/c9ra00749k. eCollection 2019 Apr 3.

Abstract

The nickel(ii)-catalyzed -arylation of unactivated C-H bonds utilizing amino acids as directing groups with aryl iodides or bromides as coupling electrophiles is described. This protocol features excellent mono-selectivity, good regioselectivity, and wide functional group tolerance. Additionally, the obtained products bearing a biaryl motif and an amino acid represent bioactive molecules with wide bioactivities.

摘要

描述了利用氨基酸作为导向基团,以芳基碘化物或溴化物作为偶联亲电试剂,通过镍(II)催化未活化C-H键的芳基化反应。该方法具有出色的单选择性、良好的区域选择性和广泛的官能团耐受性。此外,所得到的带有联芳基基序和氨基酸的产物代表了具有广泛生物活性的生物活性分子。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d23f/9062466/f985eb977430/c9ra00749k-f1.jpg

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