| 7-羟基-3,4-二氢-2(1H)喹啉酮的合成 |
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| 引用本文： | 奚小金,谢军民,王淑芬. 7-羟基-3,4-二氢-2(1H)喹啉酮的合成[J]. 化工时刊, 2008, 22(11): 26-27 |
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| 作者姓名： | 奚小金 谢军民 王淑芬 |
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| 作者单位： | 常州华生制药有限公司,江苏,常州,213000;常州华生制药有限公司,江苏,常州,213000;常州华生制药有限公司,江苏,常州,213000 |
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| 摘 要： | 目前合成7-羟基-3,4-二氢-2（1H）喹啉酮都要用到大量三氯化铝,对环境污染严重,成本较高;经过工艺改进,以少量三氟化硼乙醚溶液替代三氯化铝,以间氨基苯酚为原料,经酰化水解、傅-克烷基化两步得到7-羟基-3,4-二氢-2（1H）喹啉酮,产品纯度高,无需精制即可用于合成阿立哌唑。目标产物的结构经元素分析、质谱、氢谱、碳谱、红外光谱确证。改进后的方法操作简便、环保,适合大生产。
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| 关 键 词： | 三氟化硼 三氯化铝 喹啉酮 合成 |
Synthesis of 7-hydroxy-3,4-dihydro-1 H-quinolinone |
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| Xi Xiaojin,Xie Junming,Wang Shufen. Synthesis of 7-hydroxy-3,4-dihydro-1 H-quinolinone[J]. Chemical Industry Times, 2008, 22(11): 26-27 |
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| Authors: | Xi Xiaojin Xie Junming Wang Shufen |
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| Affiliation: | (Changzhou Watson Pharmaceutical Co. Ltd, Jiangsu Changzhou 213000) |
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| Abstract: | By replacing AICl3 with little BF3. Et2O, 7 - hydroxy - 3,4 - dihydro - 1H - quinolinone was synthesized via two steps（ acylation and hydrolyzation, F- C -alkylation） starting from m- Aminophenol. It was pure and could be used to synthesize Aripiprazole without purifying. The structure of the target compound was confirmed by elemental analysis, MS, 1HNMR, 13CNMR, IR spectra. The method improved was operation-convenient, environment -friendly and suitable for a scale production. |
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| Keywords: | BF3 AlCl3 quinolinone synthesis |
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