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【结 构 式】 
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【药物名称】Carboxyimamidate, Carbetimer, NSC-329514D, NED-137, N-137, Plimar, Polima 【化学名称】Partially imidized copolymer of ethylene and maleic anhydride 【CA登记号】82230-03-3, 74871-30-0 (former CAS registry number), 82115-75-1 (WHO;USAN) 【 分 子 式 】C23H35N5O8 【 分 子 量 】509.5641 |
【开发单位】Pfizer (Originator) 【药理作用】ONCOLYTIC DRUGS |
合成路线1
The copolymerization of ethylene (III) and maleic anhydride (II) in ethylbenzene (I) by means of benzoyl peroxide (IV) at 70 C gives an ethylene/maleic anhydride copolymer (V), which is ammoniated by treating with liquid ammonia in acetone yielding the ammoniated ethylene/maleic acid copolymer (VI). Finally, this product is imidated partially by heating in refluxing xylene.
| 【1】 Asculai, S.S.; Fields, J.E.; Johnson, R.K.; Johnson, J.H.; Carboxyimidate, a low-molecular-weight polyelectrolyte with antitumor properties and low toxixity. J Med Chem 1982, 25, 9, 1060-64. |
| 【2】 Hopkins, S.J.; Castaner, J.; Serradell, M.N.; Blancafort, P.; N-137. Drugs Fut 1983, 8, 3, 210. |
| 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) | 31977 | 1-ethylbenzene | 100-41-4 | C8H10 | 详情 | 详情 |
| (II) | 11182 | 2,5-Furandione; Maleic anhydride | 108-31-6 | C4H2O3 | 详情 | 详情 |
| (III) | 18363 | 4-chloro-2-methyl-5-(methylsulfonyl)benzoic acid | C9H9ClO4S | 详情 | 详情 | |
| (IV) | 35970 | benzoyl benzenecarboperoxoate | 94-36-0 | C14H10O4 | 详情 | 详情 |
| (V) | 35971 | 3-[2-(2,5-dioxotetrahydro-3-furanyl)ethyl]-4-(1-phenylethyl)dihydro-2,5-furandione | C18H18O6 | 详情 | 详情 | |
| (VI) | 35972 | C18H26N3O6 | 详情 | 详情 |