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filingDate 2000-09-08-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_9622f9d8c2f6f39df85b9057295e57e1
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publicationDate 2001-03-15-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber WO-0117966-A1
titleOfInvention Process for the preparation of 1-methyl-3-carbomethoxy-4-(4'-fluorophenyl)-piperidine
abstract A compound of formula (2) is prepared by treating a dispersion of crystalline arecoline hydrobromide in an organic solvent with an anhydrous strongly basic reagent to generate a solution of arecoline free base, which is reacted directly with an organometallic compound of formula (5) in which M is a Group II metal and Y a halogen or the group (I). The compound of formula (5) is typically a Grignard reagent in which M is Mg and Y is Cl or Br. The piperidine ester of structure (2) is reduced to a piperidine carbinol, coupled with sesamol, then deprotected, to give paroxetine. The process avoids the direct handling of the irritant alkaloid oil arecoline.
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type http://data.epo.org/linked-data/def/patent/Publication

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