Process for preparing levobupivacaine and analogues thereof

Details Process for preparing levobupivacaine and analogues thereof Process for preparing levobupivacaine and analogues thereof

C - Chemistry, Metallurgy

07

D

C07D 211/60 (2006.01)

Patent

CA 2200356

A process for preparing levobupivacaine, racemic bupivacaine or another N- alkyl analogue thereof, comprises chlorinating pipecolic acid hydrochloride, amidation of the resultant pipecolyl chloride hydrochloride in solvent, without isolation, with 2,6-dimethylaniline, and alkylation of the resultant pipecolic acid 2,6-xylidide. Alternatively, the alkylation may be followed by the amidation.

Procédé de préparation de lévobupivacaïne, de bupivacaïne racémique ou d'un autre analogue N-alkyle de celles-ci, comprenant la chloration d'un hydrochlorure d'acide pipécolinique, l'amination dans un solvant de l'hydrochlorure de chlorure de pipécolyle résultant, sans isolation, à l'aide de la 2,6-diméthylaniline, puis l'alcoylation du 2,6-xylidide d'acide pipécolinique résultant. Dans un autre mode de réalisation, l'alcoylation peut être suivie de l'amination.

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