【药物名称】Epanolol, ICI-141292, Visacor
化学结构式(Chemical Structure):
参考文献No.46031
标题:Alkanolamine derivatives
作者:Smith, L.H. (AstraZeneca plc)
来源:BE 0872820; FR 2412521; GB 1573359
合成路线图解说明:

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.

参考文献No.65747
标题:Epanolol
作者:Pento, J.T.; Day, B.W.
来源:Drugs Fut 1985,10(5),392
合成路线图解说明:

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.

参考文献No.607571
标题:Beta-adrenergic blocking agents. 22. 1-Phenoxy-3-[[(substituted-amido)alkyl]amino]-2-propanols
作者:Large, M.S.; Smith, L.H.
来源:J Med Chem 1982,25(11),1286
合成路线图解说明:

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.

合成路线图解说明:

The condensation of 1-(2-cyanophenoxy)-2,3-epoxypropane (I) with ethylenediamine (II) gives 1-(2-cyanophenoxy)-3-(2-aminoethylamino)-2-propanol (III), which is finally treated with phenyl isocyanate (IV) in acetonitrile.

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