TWI316938B - New phenylpiperazine derivative - Google Patents

Description

1316938 A7

1316938 A7 B7 V. INSTRUCTIONS (2 Side effects of the body's outer diameter path. The inhibitory activity of such compounds on serotonin reuptake may lead to their efficacy in behavioral patterns that are sensitive to antidepressants or anti-anxiety agents. Such compounds can be used to treat central nervous system diseases or infections caused by disruption of the dopamine system or the serotonin system, such as aggression, anxiety, autism, dizziness, depression, cognitive or memory disorders, Parkinson's disease and In particular, schizophrenia and other psychiatric diseases. It is known that the mesylate salt of the above formula is superior to its free base (such as Compound No. 89 of WO 〇 114330), and has a particularly good property. Its free base state is more soluble in water and therefore has better bioavailability. This compound has a palm center; its racemic mixture and individual mirror image isomers belong to the scope of this invention. It is an auxiliary substance for liquid or solid materials, and is made into a form suitable for oral administration by an appropriate method. The free base of this compound can be used in Europe. Prepared by the method described in Patent No. WO 0114330. The free bases are converted to the mesylate salt according to the manner in which the known salts are formed. The present invention can be illustrated by the following examples. Example: 2.0 g (4.7 mmol) The free base (prepared by the method previously described in Patent No. WO 0114330 No. 89) was dissolved in 40 ml of methanol. The suspension was heated to 60. (:, after 2 minutes, added to 0.45 g (4.7) Mm) This paper scale applies to China National Standard (CNS) A4 specification (210X297 public love:) -5 - _ 1316938 A7 B7 V. Description of invention (3) Methanesulfonic acid dissolved in 10 ml of methanol solution. The solution was clarified. Crystallization started after stirring for 5 minutes at 60 ° C. The solution was slowly cooled to 20 ° C in 60 minutes and stirred at this temperature for 30 minutes. The solution was further cooled to Celsius in 60 minutes. The mixture was stirred for 90 minutes. The obtained solid substance was separated by filtration, washed with 5 ml of methanol, and then dried under reduced pressure at 50 ° C for one night to obtain white methanesulfonic acid in a yield of 2.17 g (88%). ) -6 - This paper wave scale is suitable Chinese National Standard (CNS) A4 size (210X 297 mm)

Claims (1)

1316938 8 8 8 8 A B c D Patent application scope 1. A compound of the formula: N N-(CH2)3 .CH3SO3H 2 A pharmaceutical composition for treating diseases of the central nervous system, which comprises the compound of claim 1 as an active ingredient. 3. A compound according to claim 1 for use in the treatment of diseases of the central nervous system. This paper scale applies to the Chinese National Standard (CNS) A4 specification (210 X 297 mm)