Process for the preparation of alkylenediamine derivatives

C - Chemistry – Metallurgy – 07 – D

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260/247.7, 260/5

C07D 295/12 (2006.01) A61K 31/135 (2006.01) C07C 209/62 (2006.01) C07C 211/44 (2006.01) C07D 265/30 (2006.01)

Patent

CA 1217487

A B S T R A C T NEW PROCESS FOR THE PREPARATION OF ALKYLENEDIAMINE DERIVATIVES The invention relates to a new process for the preparation of antiarrhythmic alkylenediamine de- rivatives of general formula (I) Image (I) wherein R1 and R2 each represent independently a lower alkyl group or halogen, R3 and R4 each stand independently for hydrogen or lower alkyl group, R5 and R6 each represent independently hydrogen or a lower alkyl group, or NR5R6 may form a 5-6 membered heterocyclic group optionally contain- ing a further heteroatom, such as an oxygen, sulfur or nitrogen atom, and n is zero or one, mixtures of the above compounds, optically active forms and racemates thereof, furthermore the pharmaceutically -2- acceptable acid addition salts of the free bases, characterized by reacting a compound of general for- mula (VIb), Image (VIb) wherein R1 to R4 and n are as defined above, with an amine of general formula (III), Image (III) wherein R5 and R6 or NR5R6, respectively, are as defined above. By the process of the invention the compounds of general formula (I), possessing valuable biological properties, can be prepared in a simpler way, compared to earlier known procedures.

457184

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