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【结 构 式】 
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【分子编号】59289 【品名】(3-(3,4-dichlorophenyl)-3-{3-[4-(methylamino)-4-phenyl-1-piperidinyl]propyl}-1-piperidinyl)(phenyl)methanone 【CA登记号】 |
【 分 子 式 】C33H39Cl2N3O 【 分 子 量 】564.59768 【元素组成】C 70.2% H 6.96% Cl 12.56% N 7.44% O 2.83% |
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：(XLIII)In a further method, aminopiperidine (IV) was converted to the formamide (XL) by heating in ethyl formate. Formyl group reduction in (XL) with LiAlH4 provided the N-metyl amine (XLI). The N-benzyl group of (XLI) was then removed by catalytic hydrogenation over Pd/C. Alkylation of the resultant piperidine (XLII) with mesylate (XXVII) gave adduct (XLIII). After acetylation of (XLIII) in neat Ac2O, the racemic mixture was separated by chiral HPLC.
| 【1】 Giardina, G.A.M.; et al.; A reliable and efficient synthesis of SR 142801. Bioorg Med Chem Lett 1996, 6, 19, 2307. |
| 【2】 Grugni, M.; Rigolio, R.; Erhard, K.F. (GlaxoSmithKline Inc.; GlaxoSmithKline SpA); Process for the preparation of 3,3-disubstd. piperidines. WO 9805640 . |
| 中间体序号 | 中间体编号 | 品名 | CAS号 | 分子式 | 供应商 | 用于合成 |
|---|---|---|---|---|---|---|
| (IV) | 54994 | 1-benzyl-4-phenyl-4-piperidinylamine; 1-benzyl-4-phenyl-4-piperidinamine | C18H22N2 | 详情 | 详情 | |
| (XXVII) | 59278 | 3-[1-benzoyl-3-(3,4-dichlorophenyl)-3-piperidinyl]propyl methanesulfonate | C22H25Cl2NO4S | 详情 | 详情 | |
| (XL) | 59286 | 1-benzyl-4-phenyl-4-piperidinylformamide | C19H22N2O | 详情 | 详情 | |
| (XLI) | 59287 | 1-benzyl-N-methyl-4-phenyl-4-piperidinamine; N-(1-benzyl-4-phenyl-4-piperidinyl)-N-methylamine | C19H24N2 | 详情 | 详情 | |
| (XLII) | 59288 | N-methyl-4-phenyl-4-piperidinamine; N-methyl-N-(4-phenyl-4-piperidinyl)amine | C12H18N2 | 详情 | 详情 | |
| (XLIII) | 59289 | (3-(3,4-dichlorophenyl)-3-{3-[4-(methylamino)-4-phenyl-1-piperidinyl]propyl}-1-piperidinyl)(phenyl)methanone | C33H39Cl2N3O | 详情 | 详情 |
Extended Information