Abstract: A new process is described for obtaining 5-cyanophthalide, which is an intermediate used for the synthesis of citalopram and its active enantiomer S(+) citalopram, both of which are known active ingredients commonly used for treating depression. The process involves starting from 5-carboxyphthalide which is converted into the corresponding acylochloride. The latter is reacted with hydroxylamine to produce the corresponding hydroxamyl phthalide, which is subsequently subjected to a dehydration reaction to produce 5-cyanophthalide.
Type:
Grant
Filed:
October 13, 2006
Date of Patent:
January 27, 2009
Assignee:
Adorkem Technology SpA
Inventors:
Giovanni Cotticelli, Raul Salvetti, Marco Zappa
Abstract: A process is described for the preparation of citalopram (I) and of the active enantiomer thereof, escitalopram (II), which process comprises the cyclisation reaction of the corresponding precursor diol of the formula III or, respectively, IV in the presence of an azodicarboxylate, a phosphine and a strong base.
Abstract: A process is described for the preparation of escitalopram and the pharmaceutically acceptable salts thereof starting from 5-cyanophthalide by a process which provides an enantioselective enzymatic deacylation reaction of a complex of the formula (IV) where R represents a C1-C4 alkyl residue or an aryl residue under the action of an esterase from Aspergillus niger.
Type:
Application
Filed:
June 14, 2006
Publication date:
August 21, 2008
Applicant:
ADORKEM TECHNOLOGY SPA
Inventors:
Giovanni Cotticelli, Raul Salvetti, Chiara Bertoni
Abstract: A process is described for the preparation of citalopram (I) and of the active enantiomer thereof, escitalopram (II), which process comprises the cyclisation reaction of the corresponding precursor diol of the formula III or, respectively, IV in the presence of an azodicarboxylate, a phosphine and a strong base.
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