Resolution of...

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C - Chemistry, Metallurgy

07

C

C07C 255/43 (2006.01) C07C 253/34 (2006.01) C07C 255/41 (2006.01)

Patent

CA 2244364

A reproducible process for preparing a substantially single enantiomer (R or S) of 4-cyano-4-(3,4-dimethoxyphenyl)-5-methylhexanoic acid, or an analogue thereof, thereby providing single enantiomer acid for the first time, proceeds by means of a classical salt resolution employing a resolving agent selected from an enantiomer (R or S) of a 1-arylalkylamine and (-)-quinine, and provides novel salts that are readily convertible to verapamil.

L'invention concerne un procédé reproductible visant à préparer un enantiomère sensiblement unique (R ou S) de l'acide 4-cyano-4-(3,4-diméthoxyphényl)-5-méthylhexanoïque, ou un analogue de celui-ci, fournissant ainsi un acide enantiomère unique dans un premier temps. On effectue ce procédé au moyen d'une résolution d'un sel classique en employant un agent de résolution sélectionné à partir d'un enantiomère (R ou S) d'une 1-arylalkylamine et d'une (-)-quinine. Ce procédé fournit de nouveaux sels qui sont facilement convertibles en vérapamil.

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