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 Synthesis of Carvedilol
  • Synthesis of Carvedilol
  • (CAS NO.: ), with its systematic name of 2-Propanol, 1-(9H-carbazol-4-yloxy)-3-((2-(2-methoxyphenoxy)ethyl)amino)-, (+-)-, could be produced through many synthetic methods.

    Following are two of the reaction routes:

    Synthesis of Carvedilol

    1. 2-(2-Bromoethoxy)anisole (I) could react with benzylamine (II) to produce secondary amine (III) in the condition of heating at 80 C, and then the yielding product is condensed with epichlorohydrin (IV) by heating at 60 C to give the isopropanol derivative (V). The condensation of (V) with 4-hydroxycarbazole (VI) in the presence of K2CO3 in refluxing dioxane gives the adduct (VII), which is finally debenzylated by hydrogenolysis with H2 over Pd/C in ethanol/water.
    2. The secondary amine (III) could be condensed with 4-(2,3-epoxypropoxy)carbazole (VIII) in refluxing ethanol to produce the already reported adduct (VII), which is debenzylated as indicated.


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