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【结 构 式】 
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【分子编号】14864 【品名】N-(1-Indanyl)propargylamine; N-(2,3-dihydro-1H-inden-1-yl)-N-(2-propynyl)amine; N-(2-propynyl)-1-indanamine 【CA登记号】1875-50-9 |
【 分 子 式 】C12H13N 【 分 子 量 】171.24196 【元素组成】C 84.17% H 7.65% N 8.18% |
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：(IV)Rasagiline can be obtained by two related ways: 1) The alkylation of racemic 1-aminoindane with propagyl chloride (II) and K2CO3 in hot acetonitrile gives the racemic secondary amine (III), which is submitted to optical resolution by chromatography over Chiracel OJ and eluting with hexane/isopropanol (90:10). 2) By alkylation of (R)-1-aminoindane (IV) with propargyl chloride (or bromide) (II) as before.
| 【1】 Graul, A.; Castaner, J.; Rasagiline. Drugs Fut 1996, 21, 9, 903. |
| 【2】 Youdim, M.B.H.; Finberg, J.P.M.; Levy, R.; Sterling, J.; Lerner, D.; Berger-Paskin, T. (Teva Pharmaceutical Industries Ltd.); R-Enantiomers of N-propargyl-1-aminoindan cpds., their preparation and pharmaceutical compsns. containing them. EP 0436492; JP 1991294248; US 5453446 . |
| 【3】 Youdim, M.B.H.; Finberg, J.P.M.; Levy, R.; Sterling, J.; Lerner, D.; Berger-Paskin, T.; Yellin, H.; Veinberg, A. (Teva Pharmaceutical Industries Ltd.); R-Enantiomer of N-propargyl-1-aminoindan, salts, compsns. and uses thereof. WO 9511016 . |
| 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) | 14861 | 1-indanamine; 2,3-dihydro-1H-inden-1-ylamine; 1-Aminoindane | 34698-41-4 | C9H11N | 详情 | 详情 |
| (II) | 14862 | Propargyl chloride; 3-chloro-1-propyne | 624-65-7 | C3H3Cl | 详情 | 详情 |
| (III) | 14863 | (1R)-2,3-Dihydro-1H-inden-1-ylamine; (R)-(-)-1-Aminoindan; (1R)-2,3-Dihydro-1H-inden-1-amine | 10277-74-4 | C9H11N | 详情 | 详情 |
| (IV) | 14864 | N-(1-Indanyl)propargylamine; N-(2,3-dihydro-1H-inden-1-yl)-N-(2-propynyl)amine; N-(2-propynyl)-1-indanamine | 1875-50-9 | C12H13N | 详情 | 详情 |
Extended Information