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inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_40296d2263ac0ffd78f14af232d908ee
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publicationDate 2009-10-15-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber WO-2009087650-A3
titleOfInvention A novel process for synthesis of pregabalin from substituted cyclopropane intermediate and a process for enzymatic resolution of racemic pregabalin
abstract A novel process of preparation of racemic pregabalin from comprising an intermediate of structure III comprising reductive ring opening to form a structure IV followed few alternative routes that yield racemic pregabalin that is resolved to yield (S) + pregabalin by using chemical or enzymatic methods. A new chemical entity of structure IIIc is also disclosed as a novel intermediate. A part of the novel process also comprises a new process of producing a compound of structure VII comprising acylation of compound of structure V followed by elimination and improving a process of producing a compound of structure VII comprising reacting isovaleraldehyde with nitromethane through the compounds 4-methyl-1-nitropentan- 2-ol, 3-methyl-1-(nitromethyl)butylacetate, and 3-methyl-1-(nitromethyl)butyl acetate under suitable conditions to 4-methyl-1-nitropet-1-ene. Enzymatic processes of resolution of racemic pregabalin esters into (S) pregabalin and (R) pregabalin are also disclosed.
priorityDate 2007-10-15-04:00^^<http://www.w3.org/2001/XMLSchema#date>
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