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【结 构 式】 
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【药物名称】BMS-379224 【化学名称】2(R)-[4-(4-Cyanophenyl)thiazol-2-yl]-1(R)-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-ylmethyl)propoxymethyl dihydrogen phosphate disodium salt 【CA登记号】 【 分 子 式 】C23H18F2N5Na2O5PS 【 分 子 量 】591.44461 |
【开发单位】Bristol-Myers Squibb (Originator) 【药理作用】Antifungal Agents, ANTIINFECTIVE THERAPY, Chemical Delivery Systems, DRUG DELIVERY, Drug Delivery Systems |
合成路线1
The condensation of BMS-207147 (I) with phosphoric acid di-tert-butyl chloromethyl triester (II) by means of NaH in THF gives the phosphoric triester (III), which is finally hydrolyzed with TFA in dichloromethane and treated with Na2CO3 to provide the target disodium salt.
| 【1】 Ueda, Y.; Barbour, N.; Bronson, J.J.; et al.; BMS-379224, a water-soluble prodrug of ravuconazole. 42nd Intersci Conf Antimicrob Agents Chemother (Sept 27 2002, San Diego) 2002, Abst F-817. |
| 【2】 Hudyma, T.W.; Golik, J.; Ueda, Y.; Chen, C.-P.; Matiskella, J.D. (Bristol-Myers Squibb Co.); Water soluble prodrugs of azole cpds.. EP 1284737; US 6362172; WO 0152852 . |
| 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) | 60212 | 4-{2-[2-(2,4-difluorophenyl)-2-hydroxy-1-methyl-3-(1H-1,2,4-triazol-1-yl)propyl]-1,3-thiazol-4-yl}benzonitrile | C22H17F2N5OS | 详情 | 详情 | |
| (II) | 42239 | di(tert-butyl) chloromethyl phosphate;di-tert-butyl chloromethyl phosphate；PHOSPHORIC ACI DI-T-BUTYL EXTER CHLOROMETHYL ESTER | 229625-50-7 | C9H20ClO4P | 详情 | 详情 |
| (III) | 60217 | {[2-[4-(4-cyanophenyl)-1,3-thiazol-2-yl]-1-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-ylmethyl)propyl]oxy}methyl bis(1,1-dimethylethyl) phosphate | C31H36F2N5O5PS | 详情 | 详情 |
Extended Information