http://rdf.ncbi.nlm.nih.gov/pubchem/patent/ES-2445543-T3

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classificationIPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D311-58
filingDate 2011-02-09-04:00^^<http://www.w3.org/2001/XMLSchema#date>
grantDate 2014-03-03-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_ac939eea0edae65343672cf354116834
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_c6e92513f20c2cb01593a08283c1ecd3
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publicationDate 2014-03-03-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber ES-2445543-T3
titleOfInvention Procedure for the preparation of nebivolol
abstract Procedure for the preparation of the compound nebivolol in the form of a racemic mixture of the two enantiomers [2S [2R [R [R]]]] - α, α '- [imino-bis (methylene)] bis [6-fluoro-chroman- 2-methanol] and [2R [2S [S [S]]]] - α, α '- [imino-bis (methylene)] bis [6-fluoro-chroman-2-methanol], which have the following formulas: ** Formula ** comprising the following stages: a. react a mixture of the four SR, RS, RR and SS isomers of the epoxide of formula (1): ** Formula ** with an R-NH2 amine, in which R is a protective group selected from methyl, allyl, t-butyl, benzyl, diphenylmethyl, triphenylmethyl, fluorenyl, 9,1-dihydroanthren-9-yl, dibenzyl, in which the aromatic rings can possibly be mono- or di-substituted with a group selected from: halogen, nitro, a C1-C4 alkyl chain, CF3, CHF2, an OR2 group in which R2 is a hydrogen, a C1-C4 alkyl, in a solvent represented by a sterically restricted alcohol selected from iPrOH, sec-BuOH, tert-BuOH, isoamyl, 2-methyl-2-butanol, 2-methyl-2-pentanol, used alone or in a mixture with an apolar solvent selected from the group of petroleum ether, pentane, hexane, cyclohexane, methylcyclohexane, heptane, benzene and toluene, in order to obtain a mixture of the four compounds 2, 3, 4 and 5, from which the 2/3 pair separates from l a couple 4/5, ** Formula ** b. by reacting amines 2 and 3, in a mixture, with the pair of epoxides 4 and 5, in a mixture, in order to obtain a mixture of 4 compounds (6, 7, 8 and 9), ** Formula **
priorityDate 2010-02-11-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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