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1.发明公开PROCEDE DE PREPARATION D'UN DERIVE D'ACIDE BENZOFURANE CARBOXYLIQUE OPTIQUEMENT PUR, ET SON UTILISATION POUR PREPARER L'EFAROXAN 失效方法用于制造光学纯BENZOFURANCARBONSÄUREDERIVATES及其用途用于生产依法克生
公开(公告)号：EP0824531A1
公开(公告)日：1998-02-25
申请号：EP96919883.0
申请日：1996-05-09
发明人： IMBERT, Thierry , MAYER, Patrick
CPC分类号： C07D405/04 , C07D307/85
摘要： A novel method for preparing an optically pure 2-ethyl-2,3-dihydro-benzofurancarboxylic acid derivative of general formula (II) is described, wherein R is a hydrogen atom, a halogen, a lower alkyl, lower alkoxy or hydroxy radical. The method comprises separating the racemic mixture by selective crystallisation with the suitable optically pure enantiomer of 2-phenylglycinol, in a suitable solvent, whereafter the optically pure, crystallised acid of formula (II) is isolated and recovered. The invention also provides the optically pure 2-ethyl-2,3-dihydro-benzofurancarboxylic acid derivative thus obtained and the use thereof for the preparation of an optically pure derivative of efaroxan.
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2.发明授权PROCEDE DE PREPARATION D'UN DERIVE D'ACIDE BENZOFURANE CARBOXYLIQUE OPTIQUEMENT PUR, ET SON UTILISATION POUR PREPARER L'EFAROXAN 失效方法用于制造光学纯BENZOFURANCARBONSÄUREDERIVATES及其用途用于生产依法克生
公开(公告)号：EP0824531B1
公开(公告)日：2000-03-22
申请号：EP96919883.7
申请日：1996-05-09
发明人： IMBERT, Thierry , MAYER, Patrick
IPC分类号： C07D307/85 , C07D405/04
CPC分类号： C07D405/04 , C07D307/85
摘要： A novel method for preparing an optically pure 2-ethyl-2,3-dihydro-benzofurancarboxylic acid derivative of general formula (II) is described, wherein R is a hydrogen atom, a halogen, a lower alkyl, lower alkoxy or hydroxy radical. The method comprises separating the racemic mixture by selective crystallisation with the suitable optically pure enantiomer of 2-phenylglycinol, in a suitable solvent, whereafter the optically pure, crystallised acid of formula (II) is isolated and recovered. The invention also provides the optically pure 2-ethyl-2,3-dihydro-benzofurancarboxylic acid derivative thus obtained and the use thereof for the preparation of an optically pure derivative of efaroxan.
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