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【结 构 式】 
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【分子编号】28428 【品名】diethyl 1-(diethoxyphosphoryl)vinylphosphonate 【CA登记号】 |
【 分 子 式 】C10H22O6P2 【 分 子 量 】300.228604 【元素组成】C 40.01% H 7.39% O 31.97% P 20.63% |
与该中间体有关的原料药合成路线共 2 条
合成路线1
该中间体在本合成路线中的序号：(II)The title compound was synthesized by condensation of cyprofloxacin (I) with tetraethyl ethenylidenebisphosphonate (II) in the presence of Et3N in CH2Cl2
| 【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. |
| 【2】 Herczegh, P.; Sztaricskai, F.J.; Farcasiu, D.; Hartmann, J.F. (ElizaNor Biopharmaceuticals, Inc.); Diphosphonate derivs. of therapeutic agents. US 5880111; WO 9640190 . |
合成路线2
该中间体在本合成路线中的序号：(II)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