Wu Zhongshi
2010
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Journal
Journal of Guiyang Medical College
Abstract
Objective:To design and synthesize a key intermediate of novel molecule-targeting angiogenesis inhibitor with potent anti-tumor activity and low toxicity.Methods:2-ethyl aniline was used as starting material of the synthesis and was processed by acetic anhydride acylation,strong nitric acid nitraction at low temperature,and desacyl synthesis to produce 2-ethyl-5-nitro aniline.The product was then synthesized to 3-methyl-6-nitro-1H-indazole by using ring-closing reaction in the presence of NaNO2,and then ethylated to obtain 2,3-diethyl-6-nitro-2H-indazole.The latter compound was then reduced by SnCl2/Hcl to get target compound 2,3-diethyl-6-nitro-2H-indazole.Result:The obtained compound was identified as the target one by 1H NMR.Conclusion:The route was suitable for the preparation of 2,3-diethyl-6-nitro-2H-indazole.