Processes for the preparation of ipidacrine or ipidacrine...

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 221/16 (2006.01)

Patent

CA 2379030

A process for the preparation of ipidacrine (I) (9-amino-2,3,5,6,7,8-hexahydro- 1H-cyclopenta[b]quinoline), which comprises reacting diphosphorus pentaoxide with a trialkyl phosphate and a hydroxyl compound in a hydrocarbon solvent to thereby prepare a polyphosphoric ester having one or more free hydroxyl groups and serving as a dehydrocondensing agent and using this ester without isolation in the condensation of 2-amino-1-cyclopentene-1-carbonitrile with cyclohexanone through dehydration.

L'invention concerne un procédé de préparation d'ipidacrine (I) (9-amino-2,3,5,6,7,8-hexahydro-1H-cycopenta [b] quinoline), qui comprend un réactif d'anhydride phosphorique avec un trialkylphosphate et un composé hydroxyle dans un solvant hydrocarboné pour préparer un ester polyphosphorique présentant un ou plusieurs groupes hydroxyle libre et servant d'agent de déshydrocondensation et utilisant cet ester sans soustraction dans la condensation de 2-amino-1-cyclopentène-1-carbonitrile avec de la cyclohexanone par le biais de la déshydratation.

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