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2,3-二甲基-6-氨基-2H-吲唑的合成研究
引用本文:刘兴赋,傅晓钟,吴忠世.2,3-二甲基-6-氨基-2H-吲唑的合成研究[J].贵阳医学院学报,2010,35(1):44-46.
作者姓名:刘兴赋  傅晓钟  吴忠世
作者单位:贵阳医学院,天然药物化学教研室,贵州,贵阳,550004
摘    要:目的:设计与合成具有分子靶向性、低毒高效新型血管生成抑制剂类抗肿瘤药物中间体。方法:以2-乙基苯胺为原料经醋酐酰化、浓硝酸低温硝化及去酰基保护合成2一乙基一5.硝基苯胺,后用亚硝酸钠关环得3-甲基-6-硝基-1H-吲唑,经硫酸二甲酯甲基化得2,3-二甲基-6-硝基-2H-吲唑,最后用氯化亚锡将其还原得到目标产物,通过1^H NMR确定结构与目标产物一致。结果:所用的合成方法可靠,质量可控,总收率为15.7%。结论:所采用合成方法能用于2,3-二甲基-6-氨基-2H-吲唑的制备。

关 键 词:抗肿瘤药  2,3-二甲基-6-氨基-2H-吲唑  合成  中间体

A Study on the Synthesis of 2,3-diethyl-6-nitro-2H-indazole
LIU Xingfu,FU Xiaozhong,WU Zhongshi.A Study on the Synthesis of 2,3-diethyl-6-nitro-2H-indazole[J].Journal of Guiyang Medical College,2010,35(1):44-46.
Authors:LIU Xingfu  FU Xiaozhong  WU Zhongshi
Institution:(Department of Natural Pharmaceutical Chemistry, Guiyang Medical College, Guiyang 550004, Guizhou, China)
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 hitraction 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-2 H -indazole.
Keywords:antineoplastic agents  2  3-diethy1-6-nitro-2H-indazole  synthesis  intermediate
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