药物详细合成路线
| Name | Amlexanox;Amoxanox;CHX-3673;AA-673;OraDisc A;Aptheal;Apthera;OraRinse;Aphthasol;Elics;Solfa | | Chemical Name | 2-Amino-7-isopropyl-5-oxo-5H-[1]benzopyrano[2,3-b]pyridine-3-carboxylic acid;2-Amino-7-isopropyl-1-azaxanthone-3-carboxylic acid | | CAS | 68302-57-8 | | Related CAS | | | Formula | C16H14N2O4 | | Structure |  | | Formula Weight | 298.30098 | | Stage | 上市-1987 | | Company | Senju (Originator), Takeda (Originator), Access Pharmaceuticals (Licensee), Esteve (Licensee), GlaxoSmithKline (Licensee), Paladin (Licensee), Strakan (Licensee), Wyeth Pharmaceuticals (Licensee), Zambon (Licensee) | | Activity/Mechanism | Antiallergy/Antiasthmatic Drugs, Asthma Therapy, DERMATOLOGIC DRUGS, ONCOLYTIC DRUGS, RESPIRATORY DRUGS, Treatment of Disorders Associated with Cancer Therapy, Treatment of Mucositis, Wound-Healing Agents, Mediator Release Inhibitors | | Syn. Route | 1 | | Route 1 | | the reaction of 6-isopropyl-4-oxo-4h-1-benzopyran-3-carbonitrile (i) with morpholine (a) and dmf in hot water gives 2-amino-6-isopropyl-4-oxo-4h-1-benzopyran-3-carboxaldehyde (ii), which is cyclized with ethyl cyanoacetate (iii) by means of piperidine (b) in refluxing ethanol yielding ethyl 2-amino-7-isopropyl-1-azaxanthone-3-carboxylate (iv). finally, this compound is saponified by a treatment with sulfuric acid in refluxing acetic acid water. | | |  | | List of intermediates | No. | | 2-(benzyloxy)-4-chlorophenol | (b) | | 2-(4-benzhydryl-1-piperazinyl)ethyl (z)-2-acetyl-3-(3-nitrophenyl)-2-propenoate | (a) | | ethyl (3r)-3-hydroxy-5-(trimethylsilyl)-4-pentynoate | (iii) | | 2-chloro-5-nitrobenzenesulfonamide | (i) | | 5-nitro-2-(3-toluidino)benzenesulfonamide | (ii) | | [[bis(methylsulfanyl)methylene]amino]methane | (iv) | | | Reference 1: nohara, a.; sugihara, h.; ukawa, k. (takeda chemical industries, ltd.); 1-azaxanthone-3-carboxylic acid. be 0864647; de 2809720; fr 2383185; gb 1597024; gb 1597025; jp 78111096; jp 78111097; jp 7988298; us 4143042; us 4255576; us 4299963 . Reference 2: serradell, m.n.; castaner, j.; aa-673. drugs fut 1984, 9, 5, 311. |
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来源:药化网
作者:药化小编
摘要:本文合成路线介绍的是药物中文名氨来呫诺；英文名Amlexanox;Amoxanox;CHX-3673;AA-673;OraDisc A;Aptheal;Apthera;OraRinse;Aphthasol;Elics;Solfa；CAS[68302-57-8]
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