A practical, metal-free synthesis of 1H-indazoles

被引:90
作者
Counceller, Carla M. [1 ]
Eichman, Chad C. [1 ]
Wray, Brenda C. [1 ]
Stambuli, James P. [1 ]
机构
[1] Ohio State Univ, Dept Chem, Evans Chem Labs, Columbus, OH 43210 USA
关键词
D O I
10.1021/ol800053f
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
The synthesis of 1H-indazoles is achieved from o-aminobenzoximes by the selective activation of the oxime in the presence of the amino group. The reaction occurs with a variety of substituted o-aminobenzoximes using a slight excess of methanesulfonyl chloride and triethylamine at 0-23 degrees C and is amenable to scale-up, The synthesis of 1H-indazoles under these conditions is extremely mild compared with previous synthetic approaches and affords the desired compounds in good to excellent yields.
引用
收藏
页码:1021 / 1023
页数:3
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