| 抗炎镇痛药替尼达普钠的合成 |
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| 引用本文： | 金熔,刘嵘,王尔华.抗炎镇痛药替尼达普钠的合成[J].中国药科大学学报,2001,32(1):72-74. |
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| 作者姓名： | 金熔 刘嵘 王尔华 |
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| 作者单位： | 中国药科大学医药化工研究所， 南京 210009 |
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| 基金项目： | 国家“九五”科技攻关项目(96-902-01-07) |
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| 摘 要： | 替尼达普钠 (tenidap sodium,1 )是含吲哚结构的新型的非甾体抗炎镇痛药 ,它不仅可以抑制环氧酶 ,而且还可以抑制脂氧酶 ,调控细胞因子的活性 ,这些多重作用是以往药物所不具备的特点 ,还可以显著地快速降低急性期反应指标 ,如 C-反应蛋白、血清淀粉样蛋白、红细胞沉降率和白介素 - 6,这表明替尼达普钠具有真正有效的治疗价值 1-3]。文献报道4 -6] 以 5-氯 - 2 -氧 - 2 ,3-二氢 - 1 - H吲哚为起始原料 ,与异丙甲酰异氰酸酯反应 ,生成 1 -N- (2 ,2 -二甲基乙酰基 ) ]氨基甲酰基 - 2 -羟基 - 5-氯吲哚 ,经碱水解开环 ,生成 5-氯 - 2 -脲…
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| 关 键 词： | 替尼达普 抗炎镇痛药 合成 |
| 文章编号： | 1000-5048(2001)01-0070-03 |
| 修稿时间： | 2000年9月1日 |
Synthesis of
Anti-inflammatory and Analgesic Agents-Tenidap Sodium |
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| JIN Rong,LIU Rong,WANG Er Hua Medicinal and Chemical Institute,China Pharmaceutical University,NanJing.Synthesis of
Anti-inflammatory and Analgesic Agents-Tenidap Sodium[J].Journal of China Pharmaceutical University,2001,32(1):72-74. |
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| Authors: | JIN Rong LIU Rong WANG Er Hua Medicinal and Chemical Institute China Pharmaceutical University NanJing |
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| Institution: | JIN Rong,LIU Rong,WANG Er Hua Medicinal and Chemical Institute,China Pharmaceutical University,NanJing 210009 |
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| Abstract: | AIM: To synthesize anti inflammatory and analgesic agents Tenidap sodium. METHODS: Tenidap sodium was synthesized from 5 chloro 2 oxo 2,3 dihydro 1H indole 1 carboxamide(3) which was treated first with thenoyl chloride and then with sodium methoxide. The compound 3 was prepared from 5 chloro 2 oxindole by reacting successively with sodium methoxide, methyl chloroformate,ammonia. RESULTS: The overall yield was 30%. The structure of the product was confirmed by analysis. CONCLUSION: The reactions of all steps were carried out under very moderate conditions and suitable for a scale production. |
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| Keywords: | tenidep sodium anti inflammatory and analgesic synthesis |
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