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2-氰基苯肼合成工艺改进

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2-氰基苯肼在药物研发领域有着广泛的用途.本文提出了一种以2-卤代苯甲腈为起始原料,与肼基化合物发生取代反应得到2-氰基苯肼的新方法.通过对合成工艺的优化,选择以2-氟苯腈为原料与水合肼经一步反应得到2-氰基苯肼,其中水合肼物质的量浓度为80%,用量为2-氟苯腈的8倍时反应收率最高,为82.4%.
Improved Synthetic Process of 2-Cyanophenylhydrazine
2-cyanophenylhydrazine was widely applied in the field of drug development.In this study,the target compound was synthesized from 2-halogenated benzonitrile and hydrazine group via substitu-tion reaction.By optimizing the synthesis process,2-fluorobenzonitrile was selected as the raw material and reacting with hydrazine hydrate in one step to synthesize 2-cyanophenylhydrazine.When the con-centration of hydrazine hydrate was 80%and its dosage was 8 times of the amount of 2-fluorobenzoni-trile,2-cyanophenylhydrazine reached the highest yield of 82.4%.

2-cyanophenylhydrazineprocess research80%hydrazine hydrate2-fluorobenzonitrilesubstitution reactionsynthesis

杨加宾、张亚、苏柏朗

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南京中瑞药业有限公司,江苏南京 211100

2-氰基苯肼 工艺研究 80%水合肼 2-氟苯腈 取代反应 合成

十二五国家重大新药创制科技重大专项

2011ZX09102-003-02

2024

合成化学
四川省化学化工学会 中国科学院成都有机化学研究所

合成化学

CSTPCD
影响因子:0.42
ISSN:1005-1511
年,卷(期):2024.32(7)
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