2-(3-pyridinyl)-1h-benzimidazole derivative compound and medicament containing same

A method for producing a radioactive compound represented by the following general formula (9) or a salt thereof from a compound represented by the following general formula (3) or a salt thereof by a radiohalogenation reaction:

• wherein R1 represents a hydrogen atom or CO2Ra, R2 represents a hydrogen atom, a halogen atom or CO2Ra, R3 represents a hydrogen atom or a hydroxyalkyl group containing 1 to 10 carbon atoms, R4 represents a hydrogen atom, a hydroxy group or an alkoxy group containing 1 to 10 carbon atoms, A represents CH or a nitrogen atom, X1 and X3 each independently represent a hydrogen atom or a halogen atom, X2 represents a hydrogen atom, a halogen atom or a nitrile group, provided that at least one of X1, X2 and X3 is a halogen atom, X4 represents a radioactive halogen atom, n represents an integer of 1 to 5, and each Ra independently represents an alkyl group containing 1 to 10 carbon atoms;
• wherein R1, R2, R3, R4, A, X1, X2, X3, Ra and n are defined as above, and R6 represents a halogen atom, a substituted or unsubstituted alkylsulfonyloxy group, or a substituted or unsubstituted arylsulfonyloxy group.

A method for producing a radioactive compound represented by the following general formula (11) or a salt thereof from a compound represented by the following general formula (5) or a salt thereof by a radiohalogenation reaction:

• wherein R1 represents a hydrogen atom or CO2Ra, R2 represents a hydrogen atom, a halogen atom or CO2Ra, R3 represents a hydrogen atom or a hydroxyalkyl group containing 1 to 10 carbon atoms, R4 represents a hydrogen atom, a hydroxy group or an alkoxy group containing 1 to 10 carbon atoms, R5 represents a linear alkyl group containing 1 to 5 carbon atoms in which a hydrogen atom is optionally replaced by a halogen atom, a cyclic alkyl group containing 3 to 5 carbon atoms in which a hydrogen atom is optionally replaced by a halogen atom, a hydroxyalkyl group containing 1 to 5 carbon atoms, or an o-, p- or m-halobenzyl group, A represents CH or a nitrogen atom, X1 represents a hydrogen atom or a halogen atom, X3 represents a hydrogen atom or a halogen atom, X6 represents a radioactive halogen atom, and each Ra independently represents an alkyl group containing 1 to 10 carbon atoms;
• wherein R1, R2, R3, R4, R5, A, X1, X3 and Ra are defined as above, and R7 represents a trialkyltin group or a trialkylsilyl group.