| 11βHSD1抑制剂1-(4-氟苯甲酰基)-4-(4-三氟甲氧基苯甲酰基)哌啶的合成 |
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| 引用本文： | 刘瑛,马啸华,郝景山.11βHSD1抑制剂1-(4-氟苯甲酰基)-4-(4-三氟甲氧基苯甲酰基)哌啶的合成[J].精细化工中间体,2006,36(4):21-23. |
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| 作者姓名： | 刘瑛 马啸华 郝景山 |
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| 作者单位： | 1. 河南商丘师范学院,化学系,河南,商丘,476000
2. 河南夏邑第二高级中学,河南,夏邑,476400 |
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| 摘 要： | 以4-甲氧羰基哌啶盐酸盐(2)和氟苯甲酰氯(3)为起始原料,在三乙胺的作用下以93.5%的收率制得化合物4;化合物4甲醇水溶液,在弱碱氢氧化锂作用下,以97.8%的收率水解为化合物5;化合物5在羰基二咪唑与N-甲基-N-甲氧基盐酸盐(6)作用,以94.6%的收率制得化合物7;化合物7和4-三氟甲氧基苯基溴化镁(8)偶联,以71.8%的收率制得化合物1。四步反应总收率62.1%。
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| 关 键 词： | 哌啶衍生物 11βHSD1抑制剂 合成 |
| 文章编号： | 1009-9212(2006)04-0021-03 |
| 修稿时间： | 2006-06-30 |
Synthesis of 11βHSD1 Inhibitors 1-(4-Fluorobenzoyl)-4-(4-trifluromethoxylbenzoyl) piperidine |
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| LIU Ying,MA Xiao-hua,HAO Jing-shan.Synthesis of 11βHSD1 Inhibitors 1-(4-Fluorobenzoyl)-4-(4-trifluromethoxylbenzoyl) piperidine[J].Fine Chemical Intermediates,2006,36(4):21-23. |
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| Authors: | LIU Ying MA Xiao-hua HAO Jing-shan |
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| Affiliation: | 1. Department of Chemistry, Shangqiu Normal University, Shangqiu 476000, China; 2. Xiayi No2 High School, Xiayi 476400, China |
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| Abstract: | A Practical synthesis method of 1-(4-fluorobenzoyl)-4-(4-trifluoromethoxylbenzoyl)piperidine 1 was described. 4-Flurobenzoyl chloride 3 was treated with 1.5 equiv. of methylisonipecotate 2 in DCM in the presence of triethylamine to form compound 4 in 93.5% yield. The compound 4 then treated with aqueous LiOH to produce 5 in 97.8% yield. After the compound 5 was converted into 7 in 94.6% yield,the compound 7 then coupled with Grignard agent of compound 8 to obtain compound 1 in 71.8% yield. The overall yield of four steps was 62.1%. |
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| Keywords: | piperidine derivative 11βHSD1 inhibitors synthesis |
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