| 利培酮的合成 |
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| 引用本文： | 陆学华,潘莉,唐承卓,程卯生. 利培酮的合成[J]. 中国药物化学杂志, 2007, 17(2): 89-91 |
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| 作者姓名： | 陆学华 潘莉 唐承卓 程卯生 |
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| 作者单位： | 沈阳药科大学,制药工程学院,辽宁,沈阳,110016 |
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| 摘 要： | 目的研究利培酮的合成工艺。方法以4-哌啶甲酸为原料，经氨基保护及氯代得到1-乙氧甲酰基-4-哌啶甲酰氯（3）-3与1．3-二氟苯经傅-克酰基化、脱氨基保护、肟化、环合、成盐得到6-氟-3-（4-哌啶基）-1,2-苯并异唔唑盐酸盐（7）。7和3-（2-氯乙基）-6，7，8,9-四氢-2-甲基-4H-吡啶并[1，2-a]嘧啶-4-酮在碱催化下缩合得到利培酮（1）。结果与结论合成的利培酮经^1H-NMR、^13C-NMR、MS确证结构．总收率21．5%。该合成工艺原料价廉易得、操作简便，适合工业化生产。
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| 关 键 词： | 工艺改进 利培酮 非典型抗精神病药物 |
| 文章编号： | 1005-0108（2007）02-0089-03 |
| 收稿时间： | 2006-11-03 |
| 修稿时间： | 2006-11-03 |
Synthesis of risperidone |
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| LU Xue-hua,PAN Li,TANG Cheng-zhuo,CHENG Mao-sheng. Synthesis of risperidone[J]. Chinese Journal of Medicinal Chemistry, 2007, 17(2): 89-91 |
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| Authors: | LU Xue-hua PAN Li TANG Cheng-zhuo CHENG Mao-sheng |
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| Affiliation: | School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China |
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| Abstract: | Aim To synthesize risperidone.Methods 4-Piperidinecarboxylic acid was used as starting material to give 1-ethoxycarbinyl-4-piperidinecarbonyl chloride(3) via protection and chlorination.3 was treated with 1,3-difluorobenzene through Friedel-Crafts acylation,deprotection,oximation,cyclization and salt formation to generate the key intermediate 6-fluoro-3-(4-piperidinyl)-1,2-benzisoxazole(7),which was subjected to condensation with 3-(2-chloroethyl)-6,7,8,9-tetrahydro-2-methyl-4H-pyridopyrimidin-4-one to afford risperidone.Results and conclusion The target compound was prepared with an overall yield of 21.5% and its structure was identified by 1H-NMR,13C-NMR and MS.In view of the cheap available materials and simple operations,this synthetic process is suitable for large-scale manufacture. |
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| Keywords: | process improvement risperidone atypical antipsychotic agent |
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