| 阿立哌唑的合成 |
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| 引用本文： | 吴春艳,朱永超. 阿立哌唑的合成[J]. 中国现代药物应用, 2010, 4(1): 11-12 |
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| 作者姓名： | 吴春艳 朱永超 |
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| 作者单位： | 江苏省恩华药业股份有限公司技术中心,221007 |
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| 摘 要： | 目的合成抗精神病药阿立哌唑,并验证所用路线的中间体的螺环季铵盐结构。方法1-（2,3-二氯苯基）哌嗪盐酸盐与1,4-二溴丁烷反应后,再与7-羟基-3,4-2（1H）-喹喏啉酮反应。结果总收率达45%,目标化合物经核磁共振氢谱和红外确证结构,并验证了中间体结构,化学名为5,8-二氮杂螺[4,5]癸烷溴化物。结论此工艺路线生产成本低,反应条件温和、适宜工业化生产。并确证了中间体是5,8-二氮杂螺[4,5]癸烷溴化物,而非1-（4-溴丁基）-4-（2,3-二氯苯基）哌嗪。
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| 关 键 词： | 阿立哌唑 抗精神病药 合成 |
Synthesis of aripiprazole |
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| WU Chun-yan,ZHU Yong-chao. Synthesis of aripiprazole[J]. Chinese Journal of Modern Drug Application, 2010, 4(1): 11-12 |
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| Authors: | WU Chun-yan ZHU Yong-chao |
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| Affiliation: | .(Center of teconology,JiangSu Nhwa Pharma.Corporation,XuZhou 221007,China) |
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| Abstract: | Objective To synthesize aripiprazole,a novel antipsychotic drug.Methods aripiprazole was prepared from 1-（2,3-dichlorophenyl）piperazine hydrochloride by condensation with 1,4-dibromobutane followed by reaction with 7-hydroxy-3,4-dihydrocarbostyril.Results The overall yield was 45% aripiprazole was achieved.The process is suitable for industrial producing.the intermediate＇s structure is 8-（2,3-dichloro-phenyl）-5,8-diaza-spiro[4,5]decane bromide.Conclusion The synthetic method is economical,convenient and suitable for industrial production.It＇s proved that the intermediate＇s structure is 8-（2,3-dichloro-phenyl）-5,8-diaza-spiro[4,5]decane bromide and not 1-（4-bromo-butyl）-（2,3-dichloro-phenyl）-piperazine reported in the literature. |
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| Keywords: | Aripiprazole Antipsychotic Chemical synthesis |
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