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5—氟吲哚酮的合成研究

摘    要
5-氟吲哚酮是一种用于染料合成和抗癌药合成的中间体,其杂化分子掺入供电子原子(氮)可显著增加配基与配体间形成复合物的亲和力和选择性。5-氟吲哚酮的衍生物具有良好的生理活性,广泛应用于医药中间体的合成。本文通过两种不同的途径合成目标产物5-氟吲哚酮。方法一以对氟苯胺和水合氯醛为起始原料,先成环,再进行黄明龙还原;方法二以对氟苯胺和氯乙酰氯为起始原料,然后进行烷基化成环。本文对两种方法进行了对比分析,得出结论方法二较好。并对实验条件进行优化:1.方法二中大量的水可以改用少量多次溶解循环使用,2.方法二中温度难以控制在生产中可改用油浴控制。对产物进行了核磁及元素分析表征,确认其结构即为目标化合物5-氟吲哚酮。


关键词:5-氟吲哚酮;黄明龙还原 ;烷基化;合成

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jiaql

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5—氟吲哚酮的合成研究

摘    要
5-氟吲哚酮是一种用于染料合成和抗癌药合成的中间体,其杂化分子掺入供电子原子(氮)可显著增加配基与配体间形成复合物的亲和力和选择性。5-氟吲哚酮的衍生物具有良好的生理活性,广泛应用于医药中间体的合成。本文通过两种不同的途径合成目标产物5-氟吲哚酮。方法一以对氟苯胺和水合氯醛为起始原料,先成环,再进行黄明龙还原;
Study of 5-Fluorooxindole synthesis
Abstract
5-Fluorooxindole is an intermediate used for synthesis of dye and anticarcinogen, whose hybrid molecular  significantly increased affinity and selectivity for composition of compounds between genins and ligands due to introduction of electron donating atom(nitrogen). 5-Fluorooxindole derivates are extensively used to synthesis of pharmaceutical intermediate due to its good physiological activity. In this paper, two methods were used to produce target product. First method, p-fluoro aniline and chloral hydrate were initial materials, and ring was synthesis  first, then wolf-kishner reduction was carried out.

[ Last edited by jiaql on 2009-5-25 at 13:57 ]
2楼2009-05-25 13:53:52
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jiaql

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yjh2665091(金币+15,VIP+0):很好很强大 我这个摘要 您觉得还可以不?要不要改改? 5-26 10:22
歇一会接着来
方法二以对氟苯胺和氯乙酰氯为起始原料,然后进行烷基化成环。本文对两种方法进行了对比分析,得出结论方法二较好。并对实验条件进行优化:1.方法二中大量的水可以改用少量多次溶解循环使用,2.方法二中温度难以控制在生产中可改用油浴控制。对产物进行了核磁及元素分析表征,确认其结构即为目标化合物5-氟吲哚酮。
Second method, p-fluoro aniline and chloroacetic chloride chloroacetyl chloride were used as initial materials and alkylation was carried out. In this paper, two methods were compared and indicated that the second method was much better. In addition, experimental conditions were optimized as follows: 1. lots of water in second method could be cycled with little amount and multiple times, 2. Due to some difficulty, temperature control in second method could be substituted for oil bath. The products were characterized by means of nuclear magnetic resonance and element analysis and the structure were affirmed to accord with 5-Fluorooxindole.
3楼2009-05-25 14:21:53
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