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【结 构 式】

【分子编号】29337

【品名】N-(2-aminoethyl)-2-[4-(benzyloxy)phenyl]acetamide

【CA登记号】

【 分 子 式 】C17H20N2O2

【 分 子 量 】284.35808

【元素组成】C 71.81% H 7.09% N 9.85% O 11.25%

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:(II)

1,2-Epoxy-3-(2-cyanophenoxy)propane (I) is added to one equivalent of N-(2-aminoethyl)-4-benzyloxyphenylacetamide (II) in n-propanol and heated to reflux for 18 h, giving N-[2-(3-o-cyanophenoxy-2-hydroxypropylamino)ethyl]-4-benzyloxyphenylacetamide (III). Hydrogenolysis of the 4-benzyl moiety of (III) may be performed under mild conditions (e.g., hydrogen gas with palladium on carbon in ethanol at room temperature) to yield ICI-141292.

1 Large, M.S.; Smith, L.H.; Beta-adrenergic blocking agents. 22. 1-Phenoxy-3-[[(substituted-amido)alkyl]amino]-2-propanols. J Med Chem 1982, 25, 11, 1286.
2 Smith, L.H. (AstraZeneca plc); Alkanolamine derivatives. BE 0872820; FR 2412521; GB 1573359 .
3 Pento, J.T.; Day, B.W.; Epanolol. Drugs Fut 1985, 10, 5, 392.
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) 29336 2-(2-oxiranyloxy)benzonitrile C9H7NO2 详情 详情
(II) 29337 N-(2-aminoethyl)-2-[4-(benzyloxy)phenyl]acetamide C17H20N2O2 详情 详情
(III) 29338 1-propanol 71-23-8 C3H8O 详情 详情
(IV) 29339 2-[4-(benzyloxy)phenyl]-N-(2-[[3-(2-cyanophenoxy)-2-hydroxypropyl]amino]ethyl)acetamide C27H29N3O4 详情 详情
Extended Information