Preparation of hexahydroazepinones and hexahydroazepinoles

Details Preparation of hexahydroazepinones and hexahydroazepinoles Preparation of hexahydroazepinones and hexahydroazepinoles

C - Chemistry, Metallurgy

07

D

C07D 223/08 (2006.01) B01J 19/18 (2006.01) B01J 19/26 (2006.01) C07D 243/02 (2006.01) C07D 267/04 (2006.01) C07D 281/02 (2006.01) C07D 403/04 (2006.01)

Patent

CA 2138308

A method for the preparation of hexahydroazepinones and hexahydroazepinoles of the general formula I: Image and salts thereof, in which X signifies -N(-R)-, -CH2-, -S-, -O-, Y signifies -N (-R)-, -N (-CH3)-, -N (-CH2-CH2-C6H5)-, and Z signifies =O, -OH, wherein in each case R represents H, (C1-C5)-alkyl, (C5-C7) -cycloalkyl, (C0-C5) -alkylphenyl, by Dieckmann condensation avoiding usual dilution techniques and long reaction times. It increases the overall yields of the pharmaceutically-active compounds azelastine and flezelastine whose synthesis starts from these seven-membered heterocyclic rings.

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