Patent ID: 8273883

Claim:
A method for producing an optically active 2-arylpiperazine derivative or salt thereof, comprising steps of: treating an optically active substituted aminodiol derivative represented by the following formula (4): wherein, Ar represents an optionally substituted aryl group having 6 to 20 carbon atoms, or an optionally substituted heteroaryl group having 3 to 20 carbon atoms; R 1 represents an optionally substituted alkyl group having 1 to 20 carbon atoms, an optionally substituted cycloalkyl group having 3 to 20 carbon atoms, an optionally substituted alkenyl group having 2 to 20 carbon atoms, an optionally substituted aralkyl group having 7 to 20 carbon atoms, an optionally substituted aryl group having 6 to 20 carbon atoms, or an optionally substituted heteroaryl group having 3 to 20 carbon atoms; * indicates an asymmetric carbon atom, with a sulfonating agent in the presence of a base; and then reacting with an amine compound represented by the following formula (5): R 2 NH 2 (5) wherein, R 2 represents a hydrogen atom, an optionally substituted alkyl group having 1 to 20 carbon atoms, an optionally substituted cycloalkyl group having 3 to 20 carbon atoms, an optionally substituted alkenyl group having 2 to 20 carbon atoms, an optionally substituted aralkyl group having 7 to 20 carbon atoms, an optionally substituted aryl group having 6 to 20 carbon atoms, or an optionally substituted heteroaryl group having 3 to 20 carbon atoms; wherein, the optically active 2-arylpiperazine derivative is represented by the following formula (1): wherein, Ar, R 1 , R 2 , * mean the same as the above, and the configuration of the optically active 2-arylpiperazine derivative represented by formula (1) is S when the configuration of the optically active substituted aminodiol derivative represented by formula (4) is S, or the configuration of the optically active 2-arylpiperazine derivative represented by formula (1) is R when the configuration of the optically active substituted aminodiol derivative represented by formula (4) is R.