A novel one-pot method for the preparation of pyrazoles by 1,3-dipolar cycloadditions of diazo compounds generated in situ

被引:281
作者
Aggarwal, VK
de Vicente, J
Bonnert, RV
机构
[1] Univ Bristol, Sch Chem, Bristol BS8 ITS, Avon, England
[2] AstraZeneca R&D Charnwood, Med Chem, Loughborough LE11 5RH, Leics, England
关键词
D O I
10.1021/jo0268409
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
A convenient one-pot procedure for the preparation of pyrazoles by 1,3-dipolar cycloaddition of diazo compounds generated in situ has been developed. Diazo compounds derived from aldehydes were reacted with terminal alkynes to furnish regioselectively 3,5-disubstituted pyrazoles. Furthermore, the reaction of N-vinylimidazole and diazo compounds derived from aldehydes gave exclusively 3-substituted pyrazoles in a one-pot process.
引用
收藏
页码:5381 / 5383
页数:3
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