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【结 构 式】 
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【分子编号】44033 【品名】ethyl (E)-3-amino-4-[2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)ethoxy]-2-butenoate 【CA登记号】 |
【 分 子 式 】C16H18N2O5 【 分 子 量 】318.3294 【元素组成】C 60.37% H 5.7% N 8.8% O 25.13% |
与该中间体有关的原料药合成路线共 2 条
合成路线1
该中间体在本合成路线中的序号：(II)Preparation of a key intermediate in the synthesis of amlodipine: The reaction of ethyl 4-(2-phthalimidoethoxy)acetoacetate (I) with ammonium acetate in refluxing toluene gives the corresponding 3-aminocrotonic acid (II), which is then cyclized with methyl 2-(2-chlorobenzylidene)acetoacetate (III) in refluxing ethanol.
| 【1】 Campon Pardo, J.; Coppi, L.; Gasanz Guillen, Y. (Laboratorios del Dr. Esteve, SA); Intermediate for the synthesis of amlodipine, preparation process and corresponding utilization. WO 0024714 . |
| 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) | 44032 | Ethyl 4-(2-phthalimidoethoxy)acetoacetate;ETHYL4-[2-(1,3-DIOXO-1,3-DIHYDRO-2H-ISOINDOL-2-YL)ETHOXYL]-3-OXOBUTANOATE;Ethyl-4(2-Phthalimido Ethoxy)Acetoacetate;ethyl 4-(2-(1,3-dioxoisoindolin-2-yl)ethoxy)-3-oxobutanoate; Ethyl 4-[2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)ethoxy]-3-oxobutanoate | 88150-75-8 | C16H17NO6 | 详情 | 详情 |
| (II) | 44033 | ethyl (E)-3-amino-4-[2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)ethoxy]-2-butenoate | C16H18N2O5 | 详情 | 详情 | |
| (III) | 44034 | methyl (Z)-2-acetyl-3-(2-chlorophenyl)-2-propenoate | C12H11ClO3 | 详情 | 详情 | |
| (IV) | 44035 | Phthalimido amlodipine; Phthaloyl Amlodipine; 3-Ethyl 5-methyl 4-(2-chlorophenyl)-2-[[2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)ethoxy]methyl]-6-methyl-1,4-dihydro-3,5-pyridinedicarboxylate | 103094-30-0 | C28H27ClN2O7 | 详情 | 详情 |
合成路线2
该中间体在本合成路线中的序号：(II)
| 【1】 Coppi L,Gasanz GY,Campon PJ.Intermediate for the synthesis of amlodipine,preparation process and corresponding utilization:WO,Patent 2,000,024,714,2000. |
| 【2】 Berenguer Maimo R,Merodio Cabanillas JF,Medriano Reperez J.Acetone solvate of phthaloylamlodipine:EP,Patent 1,975,167,2008. |
| 【3】 石卫兵，赖宜生，张奕华.苯磺酸氨氯地平的合成研究.中国药物化学杂志，2006,16:161. |
| 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) | 44032 | Ethyl 4-(2-phthalimidoethoxy)acetoacetate;ETHYL4-[2-(1,3-DIOXO-1,3-DIHYDRO-2H-ISOINDOL-2-YL)ETHOXYL]-3-OXOBUTANOATE;Ethyl-4(2-Phthalimido Ethoxy)Acetoacetate;ethyl 4-(2-(1,3-dioxoisoindolin-2-yl)ethoxy)-3-oxobutanoate; Ethyl 4-[2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)ethoxy]-3-oxobutanoate | 88150-75-8 | C16H17NO6 | 详情 | 详情 |
| (II) | 44033 | ethyl (E)-3-amino-4-[2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)ethoxy]-2-butenoate | C16H18N2O5 | 详情 | 详情 | |
| (III) | 44034 | methyl (Z)-2-acetyl-3-(2-chlorophenyl)-2-propenoate | C12H11ClO3 | 详情 | 详情 | |
| (IV) | 44035 | Phthalimido amlodipine; Phthaloyl Amlodipine; 3-Ethyl 5-methyl 4-(2-chlorophenyl)-2-[[2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)ethoxy]methyl]-6-methyl-1,4-dihydro-3,5-pyridinedicarboxylate | 103094-30-0 | C28H27ClN2O7 | 详情 | 详情 |
| (V) | 69570 | Benzenesulfonic acid;Phenylsulfonic acid;Benzenemonosulfonic acid;Benzensulfonic acid;Benzenesulphonic acid; | 98-11-3 | C6H6O3S | 详情 | 详情 |
Extended Information