药物详细合成路线
| Name | Zoledronic acid monohydrate;CGP-42446(anhydrous);ZOL-446;CGP-42446A(disodium salt);CGP-42446B(triNa salt;hydrate);Zometa | | Chemical Name | 1-Hydroxy-2-(1-imidazolyl)ethylene-1,1-diphosphonic acid monohydrate | | CAS | 165800-06-6 | | Related CAS | 118072-93-8 (anhydrous), 165800-07-7 (diNa salt), 157432-59-2 (Mg salt), 131654-46-1 (Na salt), 165 | | Formula | C5H12N2O8P2 | | Structure |  | | Formula Weight | 290.10759 | | Stage | 上市-2000 | | Company | Novartis (Orphan Drug), Novartis (Originator) | | Activity/Mechanism | ANALGESIC AND ANESTHETIC DRUGS, Analgesic Drugs, Antiarthritic Drugs, Bone Cancer Therapy, Bone Diseases, Treatment of, Bone Resorption Inhibitors, METABOLIC DRUGS, Neuropathic Pain, Treatment of, Oncolytic Drugs, Rheumatoid Arthritis, Treatment of, Treatment of Hypercalcemia, TREATMENT OF MUSCULOSKELETAL & CONNECTIVE TISSUE DISEASES, Treatment of Osteoporosis, Treatment of Pagets Disease, Angiogenesis Inhibitors, Bisphosphonates | | Syn. Route | 1 | | Route 1 | | zoledronate sodium can be prepared by reaction of 2-(1-imidazolyl)acetic acid hydrochloride (i) with pcl3, with optional presence of phosphoric acid, in refluxing chlorobenzene, followed by hydrolysis with refluxing 9n hydrochloric acid and final formation of the sodium salt by treatment with aqueous naoh. | | |  | | List of intermediates | No. | | (2s)-2-amino-n,n,3,3-tetramethylbutanamide | (i) | | | Reference 1: widler, l.; et al.; highly potent geminal bisphosphonates. from pamidronate disodium (aredia) to zoledronic acid (zometa). j med chem 2002, 45, 17, 3721. Reference 2: jaeggi, k.a.; widler, l. (novartis ag); substituted alkanediphosphonic acids and pharmaceutical use. au 8781453; ep 0275821; jp 1988150291; us 4939130 . Reference 3: castaner, j.; rabasseda, x.; sorbera, l.a.; zoledronate disodium. drugs fut 2000, 25, 3, 259. |
|
来源:药化网
作者:药化小编
摘要:本文合成路线介绍的是药物中文名唑来磷酸一水化合物；英文名Zoledronic acid monohydrate;CGP-42446(anhydrous);ZOL-446;CGP-42446A(disodium salt);CGP-42446B(triNa salt;hydrate);Zometa；CAS[165800-06-6]
|
