| 第 36 卷第 4 期 |  | Vol. 36 No. 4 | | 2006 年 8 月 | Aug 2006 |
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所屬欄目：醫藥及中間體
11βHSD1抑制劑1-(4-氟苯甲�；�)-4-(4-三氟甲氧基苯甲�；�)哌啶的合成 |
| 劉瑛; 馬嘯華; 郝景山(河南商丘師范學(xué)院化學(xué)系; 河南夏邑第二高級中學(xué); 河南商丘; 河南夏邑) |
| 摘 要：以4-甲氧羰基哌啶鹽酸鹽(2)和氟苯甲酰氯(3)為起始原料,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,在弱堿氫氧化鋰作用下,以97.8%的收率水解為化合物5;化合物5在羰基二咪唑與N-甲基-N-甲氧基鹽酸鹽(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鎂(8)偶聯(lián),以71.8%的收率制得化合物1。四步反應總收率62.1%。 |
| 關(guān)鍵詞：哌啶衍生物; 11βHSD1抑制劑; 合成 |
| 中圖分類(lèi)號：TQ463+.54 文獻標識碼：A 文章編號：1009-9212(2006)04-0021-03 |
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| Synthesis of 11βHSD1 Inhibitors 1-(4-Fluorobenzoyl)-4-(4-trifluromethoxylbenzoyl)piperidine |
| LIU Ying1; MA Xiao-hua1; HAO Jing-shan2 （1. Department of Chemistry; Shangqiu Normal University; Shangqiu 476000; China; 2 . Xiayi No.2 High School; Xiayi 476400; China） |
| 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... |
| Key words：piperidine derivative; 11βHSD1 inhibitors; synthesis |
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收稿日期：2006-06-30
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