PROCESS FOR PREPARING ENTACAPONE SUBSTANTIALLY FREE OF Z-ISOMER, SYNTHESIS INTERMEDIATES THEREOF AND A NEW CRYSTALLINE FORM
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United States of America Patent
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Issued Date -
Dec 31, 2009
app pub date -
Feb 13, 2008
filing date -
Feb 13, 2007
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Abandoned
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Abstract
The present invention relates to a new method for obtaining Entacapone substantially free of Z-isomer from 3,4-dihydroxy-5-Nitrobenzaldehyde and N,N-Dimethylcyanoacetamide, or directly from a mixture of (E)- and (Z)-isomers of Entacapone, by formation of organic or inorganic salts, specially piperidine and sodium ones. A new crystalline form G of Entacapone can be obtained from this method in a fast, efficient, and simple way and substantially free of Z-isomer. Another object of the invention is a pharmaceutical composition comprising it.
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