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【结 构 式】 
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【药物名称】Pineprofen, Ibuprofen piconol, BE-100, Vesicum, Staderm 【化学名称】Ibuprofen 2-pyridylmethyl ester 【CA登记号】64622-45-3 【 分 子 式 】C19H23NO2 【 分 子 量 】297.40066 |
【开发单位】Hisamitsu (Originator), Torii (Originator) 【药理作用】DERMATOLOGIC DRUGS, Topical Antiinflammatory Agents, Cyclooxygenase-1 Inhibitors, Cyclooxygenase-2 Inhibitors, Cyclooxygenase-3 Inhibitors, Non-Steroidal Antiinflammatory Drugs |
合成路线1
This compound can be obtained in two different ways: 1) By reaction of 2-(p-isobutylphenyl)propionic acid sodium salt (I) with 2-pyridylmethyl chloride (II) in refluxing benzene. 2) By reaction of 2-(p-isobutylphenyl)propionyl chloride (III) with 2-pyridylmethanol (IV) by means of triethylamine in THF.
| 【1】 Noda, K.; Nakagawa, A.; Ishikura, Y.; Tosu, S.; Ide, H. (Hisamitsu Pharmaceutical Co., Ltd.); Pyridylalkyl esters of 2-(p-isobutylphenyl)acetic acid and propionic acids and use. US 4150137 . |
| 【2】 Castaner, J.; Blancafort, P.; Serradell, M.N.; Pineprofen. Drugs Fut 1982, 7, 6, 401. |
| 中间体序号 | 中间体编号 | 品名 | CAS号 | 分子式 | 供应商 | 用于合成 |
|---|---|---|---|---|---|---|
| (I) | 31961 | sodium 2-(4-isobutylphenyl)propanoate | C13H17NaO2 | 详情 | 详情 | |
| (II) | 26187 | 2-(Chloromethyl)pyridine | 4377-33-7 | C6H6ClN | 详情 | 详情 |
| (III) | 22117 | 2-(4-isobutylphenyl)propanoyl chloride | C13H17ClO | 详情 | 详情 | |
| (IV) | 30208 | 2-pyridinylmethanol；pyridin-2-ylmethanol；2-pyridylmethanol | 586-98-1 | C6H7NO | 详情 | 详情 |