Efficient synthesis of 3-aryl-1H-indazol-5-amine by Pd-catalyzed Suzuki-Miyaura cross-coupling reaction under microwave-assisted conditions

被引：17
作者：
Wang, Shengqiang [1 ,2 ,3 ]
Guo, Ruiyun [2 ,3 ]
Li, Jingya [2 ,3 ]
Zou, Dapeng [1 ,2 ]
Wu, Yangjie [1 ,2 ]
Wu, Yusheng [1 ,2 ,3 ,4 ]
机构：
[1] Zhengzhou Univ, Coll Chem & Mol Engn, Key Lab Chem Biol & Organ Chem Henan Prov, Zhengzhou 450052, Henan, Peoples R China
[2] Collaborat Innovat Ctr New Drug Res & Safty Evalu, Zhengzhou, Henan Province, Peoples R China
[3] Tetranov Biopharm UC, Zhengzhou 450052, Henan, Peoples R China
[4] Tetranov Int Inc, New Brunswick, NJ 08901 USA
来源：
TETRAHEDRON LETTERS | 2015年 / 56卷 / 24期
关键词：
3-Aryl-1H-indazol-5-amine; Suzuki-Miyaura cross-coupling; Microwave-assisted conditions; Arylboronic acids; RuPhos; 3-SUBSTITUTED INDAZOLES; BORONIC ACIDS; ARYNES; 1H-INDAZOLES; DERIVATIVES; INHIBITORS; ARYLATION; FUNCTIONALIZATION; PYRAZOLES; DESIGN;
D O I：
10.1016/j.tetlet.2015.04.024
中图分类号：
O62 [有机化学];
学科分类号：
070303 ; 081704 ;
摘要：
Various 3-aryl-1H-indazol-5-amine derivatives were synthesized by Pd-catalyzed Suzuki-Miyaura cross-coupling reaction of (NH) free 3-bromo-indazol-5-amine with arylboronic acids under microwave-assisted conditions. The coupling reaction can be carried out under the conditions with dioxane/H2O as solvent, Pd(OAc)(2) and RuPhos as catalyst system, and K3PO4 as a base in good to excellent yields. (C) 2015 Elsevier Ltd. All rights reserved.
引用
收藏
页码：3750 / 3753
页数：4
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