Methods for one-pot n-demethylation/n-acylation of morphine...

C - Chemistry – Metallurgy – 07 – D

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C07D 489/02 (2006.01)

Patent

CA 2692426

The present invention relates to a one-pot method for N-demethylation and/or N- acylation of a tertiary N-methylated heterocycle such as morphine alkaloids or tropane alkaloids The method, exemplified by Scheme 1, comprises reacting said tertiary N-methylated heterocycle with an acylatmg agent in the presence of a Pd metal catalyst.

La présente invention porte sur un procédé récipient unique de N-déméthylation et/ou une N-acylation d'un hétérocycle N-méthylé tertiaire tel que les alcaloïdes morphiniques ou les alcaloïdes tropaniques. Le procédé (voir Schéma 1) comporte la réaction dudit hétérocycle N-méthylé tertiaire avec un agent d'acylation en présence d'un catalyseur métallique au Pd.

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