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【结 构 式】 
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【药物名称】Nemorubicin, PNU-152243, FCE-23762 【化学名称】3'-Deamino-3'-[2(S)-methoxymorpholin-4-yl]doxorubicin 【CA登记号】108852-90-0, 108943-08-4 (HCl) 【 分 子 式 】C32H37NO13 【 分 子 量 】643.65059 |
【开发单位】Pfizer (Originator) 【药理作用】Antibiotics and Alkaloids, Antineoplastic Antibiotics, Liver Cancer Therapy, ONCOLYTIC DRUGS |
合成路线1
The oxidative cleavage of methyl beta-L-arabinopyranoside (I) with sodium periodate in water gives the dialdehyde (II), which is then cyclized with daunorubicin by means of NaHCO3 and sodium cyanoborohydride in acetonitrile/water.
| 【1】 Graul, A.; Leeson, P.; Castaner, J.; Nemorubicin. Drugs Fut 1997, 22, 12, 1239. |
| 【2】 Bargiotti, A.; Zini, P.; Penco, S.; Giuliani, F. (Pharmacia Corp.); Novel morpholino derivs. of daunorubicins and doxorubicins. BE 0904431; DE 3609052; GB 2172594; JP 1986221194; US 4672057 . |
| 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) | 11673 | (2S,3R,4S,5S)-2-Methoxytetrahydro-2H-pyran-3,4,5-triol | C6H12O5 | 详情 | 详情 | |
| (II) | 11674 | (2S)-2-Methoxy-2-(2-oxoethoxy)ethanal | C5H8O4 | 详情 | 详情 | |
| (III) | 11675 | (8S,10S)-10-[[(2R,4S,5S,6S)-4-Amino-5-hydroxy-6-methyltetrahydro-2H-pyran-2-yl]oxy]-8-glycoloyl-6,8,11-trihydroxy-1-methoxy-7,8,9,10-tetrahydro-5,12-naphthacenedione | C27H29NO11 | 详情 | 详情 |
Extended Information