Palladium-catalyzed multi-acetoxylation of 1,3-disubstituted 1H-pyrazole-5-carboxylates via direct C(sp2)-H or C(sp3)-H bond activation

被引：10

作者：

Ding, Jun ^{[1
]}

Guo, Ying ^{[1
]}

Shao, Ling-Yan ^{[1
]}

Zhao, Fei-Yi ^{[1
]}

Liao, Dao-Hua ^{[1
]}

Liu, Hong-Wei ^{[1
]}

Ji, Ya-Fei ^{[1
]}

机构：

[1] East China Univ Sci & Technol, Sch Pharm, Shanghai 200237, Peoples R China

来源：

CHINESE CHEMICAL LETTERS | 2016年 / 27卷 / 10期

基金：

中国国家自然科学基金; 高等学校博士学科点专项科研基金;

关键词：

Palladium catalysis; Functionalized pyrazoles; Multi-acetoxylation; C-H activation; Monodentate directing group; C-H ACTIVATION; UNACTIVATED C(SP(3))-H; CLAISEN CONDENSATION; ROOM-TEMPERATURE; KNORR REACTION; FUNCTIONALIZATION; OXIDATION; ARYLATION; SP(2); ACYLOXYLATION;

D O I：

10.1016/j.cclet.2016.04.007

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

A palladium-catalyzed multi-acetoxylation of 1,3-disubstituted 1H-pyrazole-5-carboxylate derivatives containing multiple potential reactive sites is described. Therein, the sequence of this process has been appropriately investigated. The protocol mainly provides the di- and tri-acetoxylated products for 1,3-diarylpyrazoles. Besides, it is found that the acetoxylation of C(sp(3))-H bond is prior to that of C(sp(2))-H bond under structurally competitive conditions. (C) 2016 Chinese Chemical Society and Institute of Materia Medica, Chinese Academy of Medical Sciences. Published by Elsevier B.V. All rights reserved.

引用

页码：1617 / 1621

页数：5

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