http://rdf.ncbi.nlm.nih.gov/pubchem/patent/WO-2016071303-A1

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filingDate 2015-11-03-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_9a31cadffaa9f0b2fefc8c5f18f672f1
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publicationDate 2016-05-12-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber WO-2016071303-A1
titleOfInvention Process for the preparation of (1s,2r)-milnacipran
abstract The invention relates to a process for the preparation of Levomilnacipran, a compound useful in the treatment of depression, comprising the following steps: a) directly converting the enantiomerically enriched form of alcohol (D) into the enantiomerically enriched form of the phthalimido derivative (C) by treatment with phthalimide in the presence of a trialkyl or triarylphosphine and of a dialkyl azodicarboxylate, formula (I) wherein the amount of phthalimide is comprised between 1 and 1.3 equivalents with respect to the molar amount of alcohol (D) used, and the amounts of both the phosphine and the azodicarboxylate are comprised, independently from each other, between 1 and 1.5 equivalents with respect to the molar amount of alcohol (D) used; b) deblocking the enantiomerically enriched form of the phthalimido derivative (C) to obtain Levomilnacipran, formula (II).
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