A Convenient Synthesis of 1-Aryl- and 2-Aryl-Substituted Indazolones via Intramolecular C-N Coupling Promoted by KOt-Bu

被引:12
作者
Wang, Wei-juan [1 ]
Chen, Jia-hua [1 ]
Chen, Zi-cong [1 ]
Zeng, Yu-feng [1 ]
Zhang, Xue-jing [1 ]
Yan, Ming [1 ]
Chan, Albert S. C. [1 ]
机构
[1] Sun Yat Sen Univ, Sch Pharmaceut Sci, Inst Drug Synth & Pharmaceut Proc, Guangzhou 510006, Guangdong, Peoples R China
来源
SYNTHESIS-STUTTGART | 2016年 / 48卷 / 20期
基金
中国国家自然科学基金;
关键词
indazolone; C-N coupling; potassium tert-butoxide; radical reaction; 2-halobenzohydrazide; KETOHEXOKINASE INHIBITORS; BIOLOGICAL EVALUATION; 1-ARYL-1H-INDAZOLES; SELECTIVITY; AMINATION; CATALYST; RECEPTOR; MURINE; SERIES;
D O I
10.1055/s-0035-1562430
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
A new method for the synthesis of 1-arylindazolones and 2-arylindazolones from N'-aryl-2-halobenzohydrazides promoted by KOt-Bu was developed. The difference of 2-halogen substituent exerted a significant effect on the distribution of the products. Two distinct reaction pathways are proposed for the generation of 1-arylindazolones and 2-arylindazolones, respectively.
引用
收藏
页码:3551 / 3558
页数:8
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