| 第 38 卷第 4 期 |  | Vol. 38 No. 4 | | 2008 年 8 月 | Aug 2008 |
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所屬欄目：醫藥及中間體
鹽酸哌羅匹隆的合成工藝改進(jìn) |
| 潘 毅，陳 蔚，陶 勇
（天津藥物研究院，天津 300193） |
| 摘 要：以順-六氫鄰苯二甲酰亞胺（2）為起始原料，經(jīng)多步反應合成鹽酸哌羅匹�。�1）。中間體3-（哌嗪-1-基）-1，2-苯并異噻唑（9）的制備采用吡啶做催化劑，收率從文獻的56.5％提高到71.4％�？偸章蕪奈墨I的46.4％提高到60.27％。合成的鹽酸哌羅匹隆經(jīng) 1H NMR、13C NMR、MS確證結構。該合成工藝原料價(jià)廉易得、操作簡(jiǎn)便、不需過(guò)柱分離，適合工業(yè)化生產(chǎn)。 |
| 關(guān)鍵詞：工藝改進(jìn)；哌羅匹��；非典型抗精神病藥物 |
| 中圖分類(lèi)號：R971+.41 文獻標識碼：A 文章編號：1009-9212（2008）04- 0031-03 |
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| An Improved Synthesis of Perospirone Hydrochloride |
| PAN Yi，CHEN Wei，TAO Yong
（Tianjin Institute of Pharmaceutical Research，Tianjin 300193，China） |
| Abstract：Perospirone hydrochloride hydrate was synthesized through multistep reactions with cis-4-tetrahydrophthalimide as starting materia. 1，3-（piperazin-1-yl）-1，2-benzisothiazole was synthesized using pyridine as the promoter and its yield was improved from 56.5％ to 71.4％. The overall yield was improved from 46.4％ to 60.27％ and its structure was identified by 1H NMR，13C NMR and MS． In view of the cheap available materials and simple operations without colunm chromatograph，this synthetic process is suitable for large-scale manufacture. |
| Key words：proces improvement；perospirone；atypical antipsychotic agent |
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作者簡(jiǎn)介：潘 毅（1973-），男，天津人，助理研究員，主要從事藥物合成研究。（E-mail：panyi1973@sina.com）
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收稿日期： 2008-06-3
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