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【结 构 式】 
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【药物名称】WP-631 【化学名称】N,N'-Phenylenebis(methylene)bis(daunomycin) dihydrochloride 【CA登记号】192708-87-5, 186131-38-4 (free base) 【 分 子 式 】C62H66Cl2N2O20 【 分 子 量 】1230.12472 |
【开发单位】M.D. Anderson Cancer Center (Originator), University of Mississippi (Originator) 【药理作用】Anthracyclines, Apoptosis Inducers, DNA-Intercalating Drugs |
合成路线1
Condensation of two molecules of daunorubicin hydrochloride (I) with a,a'-dibromo-p-xylene (II) in the presence of Na2CO3 in DMF-CH2Cl2 at room temperature afforded the bis-daunorubicin derivative, which was purified by column chromatography and precipitated as the dihydrochloride from a MeOH-Et2O solution.
| 【1】 Priebe, W.; Chaires, J.B.; Przewloka, T.; Fokt, I.; Perez-Soler, R.; Bis-anthracyclines with high activity against doxorubicin resistant tumors. EP 0971716; JP 2000506899; WO 9734612 . |
| 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) | 18698 | 7-(3-Amino-2,3,6-trideoxy-L-lyxo-hexosyloxy)-9-acetyl-7,8,9,10-tetrahydro-6,9,11-trihydroxy-4-methoxy-5,12-naphthacenequinone; (8S,10S)-8-acetyl-10-[[(2R,4S,5S,6S)-4-amino-5-hydroxy-6-methyltetrahydro-2H-pyran-2-yl]oxy]-6,8,11-trihydroxy-1-methoxy-7,8,9,10-tetrahydro-5,12-naphthacenedione; (1S,3S)-3-Acetyl-1,2,3,4,6,11-hexahydro-3,5,12-trihydroxy-10-methoxy-6,11-dioxo-1-naphthacenyl 3-amino-2,3,6-trideoxy-alpha-lyxo-hexopyranoside; Daunomycin | 20830-81-3 | C27H29NO10 | 详情 | 详情 |
| (II) | 18697 | 1,4-bis(bromomethyl)benzene | 623-24-5 | C8H8Br2 | 详情 | 详情 |
Extended Information