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【结 构 式】 
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【药物名称】ENC-41-HP 【化学名称】1-Cyclopropyl-7-[4-(2,2-diphosphonoethyl)piperazin-1-yl]-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid 【CA登记号】 【 分 子 式 】C19H24FN3O9P2 【 分 子 量 】519.36383 |
【开发单位】ElizaNor Biopharmaceuticals (Originator) 【药理作用】Antibacterial Drugs, ANTIINFECTIVE THERAPY, Bisphosphonates, Quinolones |
合成路线1
The condensation of 1-cyclopropyl-6-fluoro-4-oxo-7-(1-piperazinyl)-1,4-dihydroquinoline-3-carboxylic acid (I) with methylenediphosphonic acid tetraethyl ester (II) by means of TEA gives the addition product (III), which is finally hydrolyzed with trimethylsilyl bromide and water to afford the target diphosphonic acid.
| 【1】 Herczegh, P.; Buxton, T.B.; McPherson, J.C. III.; Kovács-Kulyassa, A.; Brewer, P.D.; Sztaricskai, F.; Stroebel, G.G.; Plowman, K.M.; Farcasiu, D.; Hartmann, J.F.; Osteoadsorptive bisphosphonate derivatives of fluoroquinolone antibacterials. J Med Chem 2002, 45, 11, 2338. |
| 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) | 22103 | 1-cyclopropyl-6-fluoro-4-oxo-7-(1-piperazinyl)-1,4-dihydro-3-quinolinecarboxylic acid | 85721-33-1 | C17H18FN3O3 | 详情 | 详情 |
| (II) | 28428 | diethyl 1-(diethoxyphosphoryl)vinylphosphonate | C10H22O6P2 | 详情 | 详情 | |
| (III) | 63172 | 7-{4-[2,2-bis(diethoxyphosphoryl)ethyl]-1-piperazinyl}-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-3-quinolinecarboxylic acid | C27H40FN3O9P2 | 详情 | 详情 |
Extended Information