Pyrroloazepine compounds

An intermediate for the production of a pharmaceutical, which is represented by the following formula (XIV) or (XIV′):

• wherein
• the dashed line indicates the presence or absence of a bond;
• and, when the bond indicated by the dashed line is present, Z2 is not present and Z1 represents a hydrogen atom but, when the bond indicated by the dashed line is absent, Z1 and Z2 both represent hydrogen atoms;
• Z1 represents a hydrogen atom and Z2 represents a hydroxyl group;
• Z1 and Z2 both represent groups SR5 in which R5 represents a substituted or unsubstituted alkyl group, a substituted or unsubstituted aralkyl group or a substituted or unsubstituted aryl group, wherein said group may be substituted with one or more of halogen atoms, alkyl groups having 1-4 carbon atoms and alkoxy groups having 1-4 carbon atoms;
• Z1 and Z2 are combined together to represent an oxygen atom, a group NOR6 in which R6 represents a hydrogen atom, a substituted or unsubstituted alkyl group, a substituted or unsubstituted aralkyl group or a substituted or unsubstituted aryl group, wherein said group may be substituted with one or more of halogen atoms, alkyl groups having 1-4 carbon atoms and alkoxy groups having 1-4 carbon atoms, or a group represented by the formula:
• in which
• G represents a substituted or unsubstituted ethylene group or a substituted or unsubstituted trimethylene group, wherein said group may be substituted with one or more of halogen atoms, alkyl groups having 1-4 carbon atoms, aryl groups having 6-14 carbon atoms, aralkyl groups having 7-22 carbon atoms and alkylidene groups having 1-4 carbon atoms;
• A represents an alkylene group, an alkenylene group or an alkynylene group
• R represents a hydrogen atom, a linear or branched alkyl group, a cycloalkyl group, a cycloalkyl-alkyl group or a substituted or unsubstituted aralkyl group, wherein said aralkyl group may be substituted with one or more of halogen atoms, alkyl groups having 1-4 carbon atoms and alkoxy groups having 1-4 carbon atoms;
• and
• X represents an eliminative groups.

A process for the preparation of a pyrroloazepine compound represented by the following formula (IIa) or (IIa′):

• wherein
• R′ represents a linear or branched alkyl group, a cycloalkyl group, a cycloalkyl-alkyl group or a substituted or unsubstituted aralkyl group, which comprises:
• reacting a β-aminopropionic acid or a derivative thereof, which is represented by the following formula (XVI):
• R′NHCH2CH2COOR7 (XVI)
• wherein
• R7 represents a hydrogen atom or a carboxyl-protecting group, and
• R′ is as defined above, with a pyrrole-3-carboxylic acid or a derivative thereof represented by the following formula (XV):
• wherein
• Q represents a hydroxyl group, an alkoxy group or an eliminative group easily replaceable by an amino group, to produce a compound represented by the following formula (XVII):
• wherein
• R′ is as defined above, and
• R7 represents a hydrogen atom or a carbonyl protecting group, and then
• subjecting the compound represented by the formula (XVII) to ring closure.

An intermediate for the production of a pharmaceutical, which is represented by the following formula (XVII):

• wherein
• R′ represents a linear or branched alkyl group, a cycloalkyl group, a cycloalkyl-alkyl group or a substituted or unsubstituted aralkyl group;
• and
• R7 represents a hydrogen atom or a carboxyl-protecting group.