The invention concerns intermediates of formula
or
wherein R5 is alkyl or alkenyl of one to ten carbons. Preferably, R5 is isobutyl.
本发明涉及式
或
其中 R5 是一至十个碳原子的烷基或烯基。R5 最好是异丁基。
SYNTHESIS OF OPTICALLY ACTIVE CYCLOHEXYLPHENYLGLYCOLIC ACID AND ITS ESTERS
申请人:Sepracor Inc.
公开号:EP1185498A2
公开(公告)日:2002-03-13
US6350714B1
申请人:——
公开号:US6350714B1
公开(公告)日:2002-02-26
[EN] SYNTHESIS OF OPTICALLY ACTIVE CYCLOHEXYLPHENYLGLYCOLIC ACID AND ITS ESTERS<br/>[FR] SYNTHESE DE L'ACIDE CYCLOHEXYLPHENYLGLYCOLIQUE, ACTIF SUR LE PLAN OPTIQUE, ET DES ESTERS DE CELUI-CI
申请人:SEPRACOR INC
公开号:WO2000023414A2
公开(公告)日:2000-04-27
A process for the preparation of optically active cyclohexylglycolate esters is described. The process utilizes carboxylic acid activation to couple (R)- or (S)-cyclohexylphenylglycolic acid (CHPGA) with 4-N,N-diethylamino butynol or other propargyl alcohol derivatives. The preparation of the hydrochloride salt is also described. In addition, a resolution process employing tyrosine methyl ester enantiomers for preparing a single enantiomer of CHPGA from racemic CHPGA is disclosed.
[EN] METHODS AND COMPOSITIONS FOR TREATING URINARY FREQUENCY AND URGENCY USING OPTICALLY PURE (S)-OXYBUTYNIN<br/>[FR] METHODES DE TRAITEMENT DE LA FREQUENCE EXAGEREE DES MICTIONS AINSI QUE LES MICTIONS IMPERIEUSES A L'AIDE DE OXYBUTYNINE-(S) OPTIQUEMENT PURE ET COMPOSITIONS A CET EFFET
申请人:SEPRACOR INC
公开号:WO2000076490A2
公开(公告)日:2000-12-21
A method for treating urinary frequency and urgency while avoiding concomitant liability of adverse effects associated with racemic oxybutynin is disclosed. The method comprises administering a therapeutically effective amount of (S)-oxybutynin, or a pharmaceutically acceptable salt thereof, substantially free of its R enantiomer. Pharmaceutical compositions comprising (S)-oxybutynin, or a pharmaceutically acceptable salt thereof, substantially free of its R enantiomer, an antibiotic and a pharmaceutically acceptable carrier are also disclosed.