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【结 构 式】 
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【分子编号】50694 【品名】tert-butyl (2S)-7-[2-(dimethylamino)-2-oxoethoxy]-1,2,3,4-tetrahydro-2-naphthalenylcarbamate 【CA登记号】 |
【 分 子 式 】C19H28N2O4 【 分 子 量 】348.4424 【元素组成】C 65.49% H 8.1% N 8.04% O 18.37% |
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：(XXIX)The optically pure (S)-amine (XXIII) was prepared as follows: Demethylation of the previously described (S)-7-methoxy-1,2,3,4-tetrahydronaphth-2-ylamine (XXVI) in concentrated HBr under reflux gave the amino naphthol (VII). After protection of the amino group of (VII) as the N-Boc derivative (XXVII), the phenolic hydroxyl was alkylated with 2-chloro-N,N-dimethylacetamide (XXVIII) to give (XXIX). Then, Boc group cleavage in (XXIX) by means of HCl in isopropanol furnished the intermediate amine (XXIII).
| 【1】 Yanagi, T.; et al.; The practical synthesis of a uterine relaxant, bis (2-{[2S)-2-({(2R)-2-hydroxy-2-[4-hydroxy-3-(2-hydroxyethyl)-phenyl]ethyl}amino)-1,2,3,4-tetrahydronaphthalen-7-yl]oxy}-N,N-dimethylacetamide)sulfate (KUR-1246). Chem Pharm Bull 2001, 49, 8, 1018. |
| 中间体序号 | 中间体编号 | 品名 | CAS号 | 分子式 | 供应商 | 用于合成 |
|---|---|---|---|---|---|---|
| (VII) | 32819 | (7S)-7-amino-5,6,7,8-tetrahydro-2-naphthalenol | C10H13NO | 详情 | 详情 | |
| (XXIII) | 50691 | 2-[[(7S)-7-amino-5,6,7,8-tetrahydro-2-naphthalenyl]oxy]-N,N-dimethylacetamide | C14H20N2O2 | 详情 | 详情 | |
| (XXVI) | 32820 | (2S)-7-methoxy-1,2,3,4-tetrahydro-2-naphthalenylamine; (2S)-7-methoxy-1,2,3,4-tetrahydro-2-naphthalenamine | C11H15NO | 详情 | 详情 | |
| (XXVII) | 32821 | tert-butyl (2S)-7-hydroxy-1,2,3,4-tetrahydro-2-naphthalenylcarbamate | C15H21NO3 | 详情 | 详情 | |
| (XXVIII) | 12998 | 2-Chloro-N,N-dimethylacetamide | 2675-89-0 | C4H8ClNO | 详情 | 详情 |
| (XXIX) | 50694 | tert-butyl (2S)-7-[2-(dimethylamino)-2-oxoethoxy]-1,2,3,4-tetrahydro-2-naphthalenylcarbamate | C19H28N2O4 | 详情 | 详情 |
Extended Information