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【结 构 式】 
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【药物名称】Risedronate sodium, NE-58095, Optinate Septimum, Benet, Optinate, Actonel 【化学名称】2-(3-Pyridinyl)-1-hydroxyethane-1,1-biphosphonate monosodium salt 【CA登记号】115436-72-1, 105462-24-6 (free acid) 【 分 子 式 】C7H10NNaO7P2 【 分 子 量 】305.09765 |
【开发单位】Procter & Gamble (Originator), Ajinomoto (Licensee), Aventis Pharma (Licensee), Lepetit (Licensee), Eisai (Codevelopment), Takeda (Codevelopment) 【药理作用】Bone Diseases, Treatment of, METABOLIC DRUGS, Prevention of Osteoporosis, Treatment of Osteoporosis, Treatment of Paget's Disease, Bisphosphonates, Farnesyl Pyrophosphate Synthase Inhibitors |
合成路线1
Risedronic acid is prepared by treatment of 2-(3-pyridyl)acetic acid (I) with a mixture of phosphorous acid and phosphorus oxychloride at reflux for 2.5 h.
| 【1】 Benedict, J.J.; Perkins, C.M. (The Procter & Gamble Co.); Pharmaceutical compsns. containing geminal diphosphonates. AU 8551534; EP 0186405; ES 8707543; JP 1995285976; JP 1997202794; US 5583122 . |
| 【2】 Mealy, N.; Castaner, J.; Prous, J.; Risedronate Sodium. Drugs Fut 1993, 18, 7, 605. |