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【结 构 式】 
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【药物名称】Guaimesal, ZAMI-635, Bronteril 【化学名称】(±)-2-(o-Methoxyphenoxy)-2-methyl-1,3-benzodioxan-4-one 【CA登记号】81674-79-5 【 分 子 式 】C16H14O5 【 分 子 量 】286.28698 |
【开发单位】Manetti Roberts (Originator) 【药理作用】Expectorants, RESPIRATORY DRUGS, Treatment of Upper Respiratory Tract Disorders |
合成路线1
Acetylsalicylic acid (I) was converted to acid chloride (II) by refluxing in a SOCl2 solution. Condensation of acid chloride (II) with guaiacol (III) either in the absence or in the presence of tertiary amines gave rise to the target orthoester derivative. Alternatively, the title compound has been prepared by treatment of acetylsalicylic acid (I) with several acid anhydrides, followed by guaiacol (III).
| 【1】 Hundewadt, M.; Senning, A.; Aspirin prodrugs: 2-Methyl-2-aryloxy-4H-1,3-benzodioxin-4-ones acting as true aspirin prodrugs. Acta Chem Scand 1990, 44, 7, 746. |
| 【2】 Quadro, G. (Dr. Lo. Zambeletti SpA); 2,4-Dioxacyclohexanone deriv.. BE 0890731; US 4358444 . |
| 【3】 Beck, C.; Preparation of 3-methyl-3-(O-methoxyphenoxy)benzo-2,4-dioxacycloheanone. GB 2101127 . |
Extended Information