New cyclopropyl derivatives, preparation method thereof and...

Details New cyclopropyl derivatives, preparation method thereof and... New cyclopropyl derivatives, preparation method thereof and...

C - Chemistry, Metallurgy

07

D

C07D 211/60 (2006.01) A61K 31/445 (2006.01)

Patent

CA 2153264

The new cyclopropyl derivatives have formula (I) wherein R is cyclopropyl or methylcyclopropyl. The preparation process comprises reacting 2,6- dibromohexanoyl chloride with 2,6-dimethylanyline in the presence of a base at 0·-25 ·C to give 2,6-dibromohexanoyl-2,6-dimethylanilide which subsequently is caused to react with R-NH2 (wherein R is as defined hereabove) at 70-100 ·C to give the cyclopropyl derivatives having formula (I). The compounds (I) can be applied as antiarithmic agents and as local anaesthetic agents.

Les nouveaux dérivés de cyclopropyle ont la formule (I) dans laquelle R représente cyclopropyle ou methylcyclopropyle. Le procédé consiste à faire réagir du chlorure de 2,6-dibromohexanoyle avec 2,6-diméthyleaniline en présence d'une base à 0-25 ~C pour donner du 2,6-dibromohexanoyl-2,6-diméthylanilide que l'on fait ensuite réagir avec R-NH¿2? (où R est tel que défini antérieurement) à 70-100 ~C pour donner les dérivés de la formule (I). Les composés (I) sont utiles comme agents antiarythmiques et comme anesthésiques locaux.

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