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【结 构 式】 
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【药物名称】Oxitropium bromide, BA-253, Oxivent 【化学名称】(3s,6R,7S,8r)-8-Ethyl-3-[(S)-tropoyloxy]-6,7-epoxytropanium bromide 【CA登记号】30286-75-0 【 分 子 式 】C19H26BrNO4 【 分 子 量 】412.32737 |
【开发单位】Boehringer Ingelheim (Originator), Nippon Boehringer Ingelheim (Originator) 【药理作用】Asthma Therapy, Chronic Obstructive Bronchitis, Agents for, Chronic Obstructive Pulmonary Diseases (COPD), Treatment of, RESPIRATORY DRUGS, Anticholinergics |
合成路线1
Compound can be prepared in three steps starting from (-)-scopalamine (hyoscine) (I) by demethylation of (-)-scopolamine with phosgene or potassium permanganate, by alkylation of the resulting (-)-norscopolamine (II) with ethylbromide (A) by means of sodium carbonate, and by quaternization of the resulting (-)-N-ethyl-norscopolamine (III) with methylbromide yielding Ba-253-BR.
| 【1】 Dharma, A.P.; Oxitropium bromide. Drugs Fut 1979, 4, 2, 117. |
| 中间体序号 | 中间体编号 | 品名 | CAS号 | 分子式 | 供应商 | 用于合成 |
|---|---|---|---|---|---|---|
| 30344 | 1-bromoethane；ethyl bromide | 74-96-4 | C2H5Br | 详情 | 详情 | |
| (I) | 33311 | (1R,2S,4R,5S)-9-methyl-3-oxa-9-azatricyclo[3.3.1.0(2,4)]non-7-yl (2S)-3-hydroxy-2-phenylpropanoate | C17H21NO4 | 详情 | 详情 | |
| (II) | 33312 | (1R,2S,4R,5S)-3-oxa-9-azatricyclo[3.3.1.0(2,4)]non-7-yl (2S)-3-hydroxy-2-phenylpropanoate | C16H19NO4 | 详情 | 详情 | |
| (III) | 33313 | (1R,2S,4R,5S)-9-ethyl-3-oxa-9-azatricyclo[3.3.1.0(2,4)]non-7-yl (2S)-3-hydroxy-2-phenylpropanoate | C18H23NO4 | 详情 | 详情 |