Methods for the preparation of Entacapone

Organic compounds -- part of the class 532-570 series – Organic compounds – Nitriles

Reexamination Certificate

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C564S167000

Reexamination Certificate

active

07385072

ABSTRACT:
The invention disclosed in this application relates to an improved process for the preparation of Entacapone. In one embodiment the process involves: (i) reacting a 3-alkoxy-4-hydroxy-5-nitrobenzadehyde with N,N-diethylaminocyanoacetamide in the presence of a mild acid catalyst and a solvent, to provide a 3-O-alkylated Entacapone, and treating the 3-O-alkylated Entacapone with an acid catalyst in the presence of an organic base to provide Entacapone.

REFERENCES:
patent: 4963590 (1990-10-01), Backstrom et al.
Wikeberg et al, Drug metabolism and Disposition, vol. 21, No. 1, pp. 81-92, 1993.

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