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【结 构 式】 
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【分子编号】58591 【品名】N-[4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthalenyl]-N-methylamine; 4-(3,4-dichlorophenyl)-N-methyl-1,2,3,4-tetrahydro-1-naphthalenamine 【CA登记号】 |
【 分 子 式 】C17H17Cl2N 【 分 子 量 】306.23412 【元素组成】C 66.68% H 5.6% Cl 23.15% N 4.57% |
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 reaction of 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydronaphthalen-1-one (I) with methylamine by means of TiCl4 in toluene gives the corresponding imine (II), which is reduced with H2 over 5% Pd/graphite, yielding a 12:1 mixture of (??(cis)(III) and (?)(trans)(III). This mixture was resolved by a treatment with (D)-mandelic acid, crystallization of the resulting salt, and treatment with NaOH in toluene/water to afford the target (+)(S,S)(cis)-sertraline.
| 【1】 Gershon, N.; Nidam, T.; Mendelovich, M.; Pilarsky, G. (Teva Pharmaceutical Industries Ltd.; Teva Pharmaceuticals USA, Inc.); Novel process for preparing (+)-cis-sertraline. WO 0168566 . |
| 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) | 30583 | 4-(3,4-dichlorophenyl)-3,4-dihydro-1(2H)-naphthalenone; 4-(3',4'-Dichlorophenyl)-1-tetralone | 79580-19-3 | C16H12Cl2O | 详情 | 详情 |
| (II) | 30584 | N-[4-(3,4-dichlorophenyl)-3,4-dihydro-1(2H)-naphthalenylidene]-N-methylamine; N-[4-(3,4-dichlorophenyl)-3,4-dihydro-1(2H)-naphthalenylidene]methanamine | C17H15Cl2N | 详情 | 详情 | |
| (III) | 58591 | N-[4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthalenyl]-N-methylamine; 4-(3,4-dichlorophenyl)-N-methyl-1,2,3,4-tetrahydro-1-naphthalenamine | C17H17Cl2N | 详情 | 详情 |
Extended Information