Process for the preparation of diacerein

Details Process for the preparation of diacerein Process for the preparation of diacerein

1995-01-23

1997-09-23

Dees, Jose G.

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

Organic compounds

Carboxylic acid esters

560239, 560131, 552262, C07F 902, C07C33300, C07C 49593

Patent

active

056706952

ABSTRACT:
The present invention relates to a process for the preparation of 1,8-diacetoxy-3-carboxyanthraquinone, also known as diacerein, via aloin acetylation, oxidation of the acetylated product, and purification of the raw diacerein obtained by means of crystallization from 2-methoxyethanol or N,N-dimethylacetamide and optionally by dissolution of the corresponding salt with triethylamine in methylene chloride, followed by removal of the insoluble residue.

REFERENCES:
patent: 4244968 (1981-01-01), Friedmann
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patent: 4950687 (1990-08-01), Dall'Asta et al.
patent: 5391775 (1995-02-01), Carcasona et al.
patent: 5393898 (1995-02-01), Carcasona et al.
Sostanze Farmaceutiche, Axel Kleemann-Jurgen Engel, Organizzazione Editoriale Medico Farmaceutica, S.r.l. 1988.
The Merck Index, 11 Ed., Merck & Co., Inc. 1989, pp. 467, 351, 1300.
Advanced Organic Chemistry--Reactions, Mechanisms and Structure, J. March, John Wiley & Sons, 3rd Ed., 1985, pp. 346-347 and 1084.
Fairbairn et al., J. Pharm. Sci., 66 (9), pp. 1300-1303 (1977).

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