Selective N7 Alkylation of 7-Azaindazoles

A general and mild procedure for alkylation of 7-azaindazoles at the N7 position using alkyl halides in butanone is reported, which requires no additives such as acids or bases. The scope of the reaction regarding substituents on 7-azaindazoles and the alkyl electrophiles is presented.

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Bibliographic Details
Published in:Journal of organic chemistry 2020-06, Vol.85 (11), p.7558-7564
Main Authors: Lei, Zhiyu, Bao, Jianming, Cheng, Chen, Yu, Wensheng, Hu, Bin, Jin, Weichen, Jabri, Salman, Yang, Song, Zhao, Lianyun, Sinz, Christopher J, Duffy, Joseph L
Format: Article
Language:English
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Summary:A general and mild procedure for alkylation of 7-azaindazoles at the N7 position using alkyl halides in butanone is reported, which requires no additives such as acids or bases. The scope of the reaction regarding substituents on 7-azaindazoles and the alkyl electrophiles is presented.
ISSN:0022-3263
1520-6904
DOI:10.1021/acs.joc.0c00722