http://rdf.ncbi.nlm.nih.gov/pubchem/patent/WO-2008145075-A3

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classificationCPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D295-088
classificationIPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D295-088
filingDate 2008-05-28-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_ec7a0a163550d03fd558c417089ebb1b
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_efe46c77517c2bcce2677eb4baf574df
publicationDate 2009-03-19-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber WO-2008145075-A3
titleOfInvention Method for the preparation of lasofoxifene and crystalline intermediates used therein
abstract A method of preparing (-)-cis-(5R,6S)-6-phenyl-5-[4-(2-pyrrolidin-1-ylethoxy)phenyl]- 5,6,7,8-tetrahydronaphthalen-2-ol D-tartrate - lasofoxifene of formula 1, comprising the following steps a) Preparation of cis-1- {2-[4-(2-phenyl-6-methoxy- 1,2,3,4-tetrahydronaphthalen-1-yl)-phenoxy]ethyl}pyrrolidine of formula (3) by alkylation of cis-1-(4-hydroxyphenyl)-2-phenyl-6-methoxy- 1,2,3,4-tetrahydronaphthalene with 1-(2-chloroethyl)pyrrolidine base or its salt, b) Deprotection of the hydroxyl group in the substance of formula (3) by the effect of hydrobromic acid generating cis-6-phenyl-5-[4-(2-pyrrolidin-1-ylethoxy)phenyl]-5,6,7,8-tetrahydronaphthalen-2-ol hydrobromide of formula (2a), c) Conversion of the substance of formula (2a) into cis-6-phenyl-5-[4-(2-pyrrolidin-1- ylethoxy)phenyl]-5,6,7,8-tetrahydronaphthalen-2-ol of formula (2b), d) Preparation of lasofoxifene of formula (1) by conversion into the corresponding diasteroisomer by reaction with D-tartaric acid and crystallization.
priorityDate 2007-05-29-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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