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【结 构 式】 
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【分子编号】15861 【品名】tert-butyl N-[(1R,8R)-1,8,12,12-tetramethyl-2,7,10-trioxo-11-oxa-3,6,9-triazatridec-1-yl]carbamate 【CA登记号】 |
【 分 子 式 】C18H34N4O6 【 分 子 量 】402.49132 【元素组成】C 53.71% H 8.51% N 13.92% O 23.85% |
与该中间体有关的原料药合成路线共 1 条
合成路线1
该中间体在本合成路线中的序号：(III)The condensation of tert-butoxycarbonyl-D-alanine (I) with ethylenediamine (II) gives the corresponding protected diamide (III), which is deprotected in acidic medium to the diamide (IV). The reduction of (IV) with diborane in THF yields the (R,R)-4,7-diazadecane-2,9-diamine (V), which is finally condensed with 3-nitronaphthalene-1,8-dicarboxylic acid anhydride (VI) in refluxing ethanol and salified with methanesulfonic acid.
| 【1】 Robinson, C.P.; Robinson, K.A.; Castaner, J.; Bisnafide Mesylate. Drugs Fut 1996, 21, 3, 239. |
| 【2】 Sun, J.-H. (DuPont Pharmaceuticals Co.); Bis-naphthalimides containing amino-acid derived linkers as anticancer agents. EP 0506008; EP 0577753; JP 1994506229; US 5206249; WO 9217453 . |
| 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) | 15859 | Boc-D-Alanine; (2R)-2-[(tert-butoxycarbonyl)amino]propionic acid | 7764-95-6 | C8H15NO4 | 详情 | 详情 |
| (II) | 14754 | ethylenediamine;1,2-Diaminoethane;ethane-1,2-diamine；1,2-Ethanediamine | 107-15-3 | C2H8N2 | 详情 | 详情 |
| (III) | 15861 | tert-butyl N-[(1R,8R)-1,8,12,12-tetramethyl-2,7,10-trioxo-11-oxa-3,6,9-triazatridec-1-yl]carbamate | C18H34N4O6 | 详情 | 详情 | |
| (IV) | 15862 | (2R)-2-amino-N-(2-[[(2R)-2-aminopropanoyl]amino]ethyl)propanamide | C8H18N4O2 | 详情 | 详情 | |
| (V) | 15863 | (2R)-N(1)-(2-[[(2R)-2-aminopropyl]amino]ethyl)-1,2-propanediamine; N-[(2R)-2-aminopropyl]-N-(2-[[(2R)-2-aminopropyl]amino]ethyl)amine | C8H22N4 | 详情 | 详情 | |
| (VI) | 15864 | 5-nitro-1H,3H-benzo[de]isochromene-1,3-dione; 3-Nitro-1,8-naphthalic anhydride | 3027-38-1 | C12H5NO5 | 详情 | 详情 |
Extended Information