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【结 构 式】 
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【药物名称】Bemesetron, MDL-72222 【化学名称】1alphaH,3alpha,5alphaH-Tropan-3-yl-3,5-dichlorobenzoate 【CA登记号】40796-97-2 【 分 子 式 】C15H17Cl2NO2 【 分 子 量 】314.21424 |
【开发单位】Aventis Pharma (Originator) 【药理作用】ANALGESIC AND ANESTHETIC DRUGS, Antimigraine Drugs, Nausea and Vomiting, Treatment of, NEUROLOGIC DRUGS, 5-HT3 Antagonists |
合成路线1
The synthesis of [11C]-labeled MDL-72222 for use in PET studies of the 5-HT3 receptor by methylation of 3,5-dichlorobenzoic acid 8-azabicyclo[3.2.1]oct-3-yl ester (I) with [11C]-labeled methyl iodide in hot acetonitrile has been described.
| 【1】 Lasne, M.C.; Debruyne, D.; Moulin, M.; Baron, J.C.; Camsonne, R.; Barre, L.; Bonvento, G.; Gourand, F.; Synthesis and regional rat brain distribution of [C-11]MDL 72222 - A 5HT3 receptor antagonist. Appl Radiat Isot - Int J Radiat Appl Instrum Part A 1992, 43, 4, 509. |
| 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) | 10371 | (1R,5S)-8-azabicyclo[3.2.1]oct-3-yl 3,5-dichlorobenzoate | C14H15Cl2NO2 | 详情 | 详情 |
合成路线2
By reaction of tropine (I) with 3,5-dichlorobenzoyl chloride (II) at 140 C.
| 【1】 Fozard, J.R.; Gittos, M.W. (Aventis Pharma SA); Treatment og migraine with substituted tropyl benzoate derivatives. EP 0067770; JP 58000978 . |
| 【2】 Pento, J.T.; Castaner, J.; Serradell, M.N.; MDL-72222. Drugs Fut 1985, 10, 10, 820. |
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