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【结 构 式】 
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【药物名称】Roxithromycin, RU-965, RU-28965, Rossitrol, Overall, Assoral, Rulid 【化学名称】Erythromycin 9-[O-(2-methoxyethoxy)methyloxime] 【CA登记号】80214-83-1 【 分 子 式 】C41H76N2O15 【 分 子 量 】837.06727 |
【开发单位】Aventis Pharma (Originator), Camillo Corvi (Originator), Eisai (Licensee) 【药理作用】Acne Therapy, Antibacterial Drugs, Antibiotics, ANTIINFECTIVE THERAPY, DERMATOLOGIC DRUGS, Macrolides |
合成路线1
By condensation of erythromycin oxime (II) [obtained from erythromycin (I) and hydroxylamine hydrochloride] with (2 methoxyethoxy)methyl chloride (III) in the presence of NaHCO3 in refluxing acetone.
| 【1】 Gouin D'Ambrieres, S.; Chantot, J.F.; Gasc, J.C.; Lutz, A.; New ether oxime derivatives of erythromycin A: Preparation and antibacterial activities. 23rd Intersci Conf Antimicrob Agents Chemother (Oct 24-26, Las Vegas) 1983, Abst 447. |
| 【2】 Gouin, A.S.; Lutz, A.; Gasc, J.-C. (Aventis Pharmaceuticals, Inc.); Novel erythromycin a derivatives. EP 0033255; FR 2473525; JP 81100799; US 4349545 . |
| 【3】 Castaner, J.; Prous, J.; Roxithromycin. Drugs Fut 1986, 11, 9, 767. |
| 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) | 24317 | (4R,5R,6R,7S,9R,11R,12R,13S,14R)-6-[[(3R)-4-(dimethylamino)-3-hydroxy-6-methyltetrahydro-2H-pyran-2-yl]oxy]-14-ethyl-7,12,13-trihydroxy-4-[[(2R,4R,5S)-5-hydroxy-4-methoxy-4,6-dimethyltetrahydro-2H-pyran-2-yl]oxy]-5,7,9,11,13-pentamethyl-2,10-oxacycl | C36H65NO13 | 详情 | 详情 | |
| (II) | 24318 | (4R,5R,6R,7S,9R,11S,12R,13S,14R)-6-[[(3R)-4-(dimethylamino)-3-hydroxy-6-methyltetrahydro-2H-pyran-2-yl]oxy]-14-ethyl-7,12,13-trihydroxy-4-[[(2R,4R,5S)-5-hydroxy-4-methoxy-4,6-dimethyltetrahydro-2H-pyran-2-yl]oxy]-5,7,9,11,13-pentamethyl-2,10-oxacycl | C36H66N2O13 | 详情 | 详情 | |
| (III) | 40670 | 2-(chloromethoxy)ethyl methyl ether; 1-(chloromethoxy)-2-methoxyethane; (2-methoxyethoxy)methyl chloride | 3970-21-6 | C4H9ClO2 | 详情 | 详情 |
Extended Information