PREPARATION METHOD FOR FUSED PYRAZOLE-TYPE COMPOUND

The present disclosure provides a one-pot method for preparing a fused pyrazole-type compound substituted at nitrogen on 2-position, specifically an indazole-type compound substituted at nitrogen on 2-position. In the method, after azidizing a halogen in a substrate, without post-processing, R-NH2 c...

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Bibliographische Detailangaben
Hauptverfasser: WANG, Chaodong, FU, Shikang, TIAN, Yong, YE, Guozhong, SUN, Zongguo, CHEN, Yongkai
Format: Patent
Sprache:eng ; fre ; ger
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Zusammenfassung:The present disclosure provides a one-pot method for preparing a fused pyrazole-type compound substituted at nitrogen on 2-position, specifically an indazole-type compound substituted at nitrogen on 2-position. In the method, after azidizing a halogen in a substrate, without post-processing, R-NH2 can be directly added to proceed a ring-closing reaction with an aldehyde group, so as to give the fused pyrazole-type compound substituted at nitrogen on 2-position. For example, by using 2-fluoro-4 methoxy-5-nitro benzaldehyde as a raw material, the indazole-type compound substituted at nitrogen on 2-position can be obtained via azidation and ring-closing steps, and then a series of indazole derivatives can be produced by means of a hydrogenation reaction and a condensation reaction. The present method is convenient, easy to operate, and generally applicable to various substrate structures, thereby suitable for large-scale production.