Patent ID: 8258302
Filing Date: 2012-09-04
Classification: C07C,C07D

Abstract:
1. A method for producing a benzazepinone represented by formula (2), or a salt thereof, which comprises: opening a ring of an isoquinoline derivative represented by formula (1) by reaction of the isoquinoline derivative with an amine or a salt thereof; and subsequently converting the thus generated amine into a benzazepinone through a lactamization reaction by heating the amine in a solvent; wherein formula (1) is wherein R 1 represents an alkoxy group; each of R 2 to R 5 independently represents a hydrogen atom, an alkoxy group, or an alkyl group containing 1 to 10 carbon atoms; X represents an ethylene group or an arylene group; and Q is a tertiary or quaternary nitrogen atom, which, in those cases of a quaternary form, is substituted with an alkyl group or an aryl group containing 1 to 10 carbon atoms and has counter ion(s) Y − , wherein Y − represents a halide ion, an inorganic acid ion, an alkylsulfate ion, a mesylate ion, a tosylate ion, an alkylsulfonate ion, an organic acid ion, and/or a hydroxide ion; and formula (2) is wherein R 2 to R 5 and X have the same definitions as described above; R 6 represents a hydrogen atom, a hydroxyl group, an alkoxy group, an aryloxy group, an amino group, or an alkyl group or an aryl group containing 1 to 10 carbon atoms; and R 7 represents a hydrogen atom or an alkyl group containing 1 to 10 carbon atoms.