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【结 构 式】 
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【分子编号】60942 【品名】3-(4-bromophenyl)-3-hydroxy-N-methyl-3-(3-pyridinyl)propanamide 【CA登记号】 |
【 分 子 式 】C15H15BrN2O2 【 分 子 量 】335.20038 【元素组成】C 53.75% H 4.51% Br 23.84% N 8.36% O 9.55% |
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：(VI)The condensation of 4-bromophenyl-3-pyridyl ketone (I) with ethyl bromoacetate (II) by means of Zn in refluxing benzene gives ethyl 3-hydroxy-3-(3-pyridyl)-3-(4-bromophenyl)propionate (III), which is converted into the corresponding methylamide (VI) by treatment with methylamine (V) in ethanol. This compound is reduced with NaBH4 in THF yielding 3-(3-pyridyl)-3-(4-bromophenyl)-3-hydroxy-N-methylpropylamine (VII), which is finally dehydrated by treatment with 50% H2SO4 at 110 C
| 【1】 Blancafort, P.; Serradell, M.N.; Castaner, J.; Sweetman, A.J.; Nomelidine. Drugs Fut 1979, 4, 12, 885. |
| 【2】 Carlsson, P.A.E.; et al. (Astra Lakemedel AB); BE 835802; DD 122528; DE 2550005; FR 2291751; JP 7676278; NL 7513648; ZA 7506893 . |
| 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) | 60939 | (4-bromophenyl)(3-pyridinyl)methanone | C12H8BrNO | 详情 | 详情 | |
| (II) | 16640 | Ethyl 2-bromoacetate; Ethyl bromoacetate | 105-36-2 | C4H7BrO2 | 详情 | 详情 |
| (III) | 60940 | ethyl 3-(4-bromophenyl)-3-hydroxy-3-(3-pyridinyl)propanoate | C16H16BrNO3 | 详情 | 详情 | |
| (V) | 11021 | Methanamine; Methylamine | 74-89-5 | CH5N | 详情 | 详情 |
| (VI) | 60942 | 3-(4-bromophenyl)-3-hydroxy-N-methyl-3-(3-pyridinyl)propanamide | C15H15BrN2O2 | 详情 | 详情 | |
| (VII) | 60943 | 1-(4-bromophenyl)-3-(methylamino)-1-(3-pyridinyl)-1-propanol | C15H17BrN2O | 详情 | 详情 |
Extended Information