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【结 构 式】 
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【药物名称】 【化学名称】N-(Benzyloxycarbonyl)-L-valyl-N1-[4-[4-[(5R,5aR,8aR,9S)-9-[(2R,4aR,6R,7R,8R,8aS)-7,8-dihydroxy-2-methylperhydropyrano[3,2-d][1,3]dioxin-6-yloxy]-6-oxo-5,5a,6,8,8a,9-hexahydrofuro[3',4':6,7]naphtho[2,3-d][1,3]dioxol-5-yl]-2,6-dimethoxyphenoxymethyl]phenyl]-N5-carbamoyl-L-ornithinamide 【CA登记号】 【 分 子 式 】C55H65N5O18 【 分 子 量 】1084.154 |
【开发单位】Seattle Genetics (Originator) 【药理作用】Chemical Delivery Systems, DRUG DELIVERY, Drug Delivery Systems, ONCOLYTIC DRUGS, Epipodophyllotoxins |
合成路线1
The title prodrug has been obtained by condensation of the peptide (I) with etoposide (II) by means of PPh3 and DIAD in DMF.
| 【1】 Toki, B.E.; et al.; Protease-mediated fragmentation of p-amidobenzyl ethers: A new strategy for the activation of anticancer prodrugs. J Org Chem 2002, 67, 6, 1866. |
| 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) | 53571 | benzyl (1S)-1-{[((1S)-4-[(aminocarbonyl)amino]-1-{[4-(hydroxymethyl)anilino]carbonyl}butyl)amino]carbonyl}-2-methylpropylcarbamate | n/a | C26H35N5O6 | 详情 | 详情 |
| (II) | 13041 | Etoposide; (5R,5aR,8aR,9S)-9-[[(2R,4aR,6R,7R,8R,8aS)-7,8-Dihydroxy-2-methylhexahydropyrano[3,2-d][1,3]dioxin-6-yl]oxy]-5-(4-hydroxy-3,5-dimethoxyphenyl)-5,8,8a,9-tetrahydrofuro[3',4':6,7]naphtho[2,3-d][1,3]dioxol-6(5aH)-one | 33419-42-0 | C29H32O13 | 详情 | 详情 |