| 1-(4-三氟甲氧基苯甲酰基)-4-(4-甲氧基苯甲酰基)哌啶的合成研究 |
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| 引用本文： | 刘瑛,马啸华,薛嵩. 1-(4-三氟甲氧基苯甲酰基)-4-(4-甲氧基苯甲酰基)哌啶的合成研究[J]. 化工时刊, 2006, 20(8): 44-46 |
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| 作者姓名： | 刘瑛 马啸华 薛嵩 |
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| 作者单位： | 1. 商丘师范学院化学系,河南,商丘,476000
2. 北方氯碱集团,江苏,徐州,221007 |
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| 摘 要： | 以4-甲氧羰基哌啶盐酸盐(2)和对三氟甲氧基苯甲酰氯(3)为起始原料,在三乙胺的作用下以92.7%的收率制得化合物(4);化合物(4)甲醇水溶液中,在弱碱氢氧化锂作用下,以95.4%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-甲氧基盐酸盐作用,以94.2%的收率制得化合物(6);化合物(6)和4-甲氧基苯基溴化镁偶联,以60.1%的收率制得化合物(1)。4步反应总收率50.0%。
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| 关 键 词： | 哌啶衍生物 11βHSD1抑制剂 合成 |
| 收稿时间： | 2006-07-10 |
| 修稿时间： | 2006-07-10 |
Synthesis of llβHSD1 Inhibitors 1-(4-trifiuromethoxylbenzoyi)-4-(4-methoxylbenzoyi)piperidine |
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| Liu Ying,Ma Xiaohua,Xue Song. Synthesis of llβHSD1 Inhibitors 1-(4-trifiuromethoxylbenzoyi)-4-(4-methoxylbenzoyi)piperidine[J]. Chemical Industry Times, 2006, 20(8): 44-46 |
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| Authors: | Liu Ying Ma Xiaohua Xue Song |
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| Abstract: | A Practical synthesis of 1-(4-trifiuromethoxylbenzoyl)-4-(4-methoxylbenzoyl)piperidine(1)was described.4-trifluromethoxylbenzoyl chloride(3) was treated with 1.5 equiv,of methylisonipeeotate(2) in DCM in the presence of triethylamine to form compound(4) in 92.7% yield.The compound(4)then treated with aqueous LiOH to produce(5) in 95.4% yield.After the compound(5) was converted into(6) in 94.2% yield,the compound (6) then coupled with Grignard agent of compound(7) to obtain compound(1) in 60.1% yield. |
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