Taisho Pharmaceutical Co., Ltd.

Minoru Moriya

Hiroshi Ohta

Shuji Yamamoto

Kumi Abe

Yuko Araki

Xiang-Min Sun

Kazunari Sakagami

Akito Yasuhara

Hiroki Urabe

Yohei Kobashi

Yohei Matsuda

Norikazu Otake

Daisuke Matsuda

Daisuke Wakasugi

Hideaki Tabuse

Rie Shimono

Tomokazu Tamaoki

A novel process for producing optically active 2-(2-fluorobiphenyl-4-yl)propanoic acid is disclosed. This production process is characterized in that a compound of formula [1] is reacted with magnesium and so forth to prepare an organometallic reagent, which is reacted with a compound of formula [2] in the presence of a catalytic amount of a nickel compound and a catalytic amount of an optically active compound of formula [3] to obtain a compound represented by formula [4] which is subsequently converted to a compound represented by formula [5] or a pharmaceutically acceptable salt thereof. 

Method for producing optically active 2-(2-fluorobiphenyl-4-yl) propanoic acid

The present invention relates to novel compounds of formula [I] or pharmaceutically acceptable salts thereof: The compounds of the present invention are useful in the prevention or treatment of diseases such as schizophrenia, Alzheimer's disease, cognitive impairment, dementia, anxiety disorders (e.g., generalized anxiety disorder, panic disorder, obsessive-compulsive disorder, social anxiety disorder, post-traumatic stress disorder, specific phobias, acute stress disorder), depression, drug dependence, spasm, tremor, pain, Parkinson's disease, attention deficit hyperactivity disorder, bipolar disorder, eating disorder, or sleep disorders, which is based on the glycine uptake-inhibiting action.

Glycine transporter-inhibiting substances

The present invention aims to provide novel compounds of formula [I] or pharmaceutically acceptable salts thereof that are based on a glycine uptake inhibiting action and which are useful in the prevention or treatment of such diseases as schizophrenia, Alzheimer's disease, cognitive dysfunction, dementia, anxiety disorders (generalized anxiety disorder, panic disorder, obsessive-compulsive disorder, social anxiety disorder, posttraumatic stress disorder, specific phobia, acute stress disorder, etc.), depression, drug addiction, spasm, tremor, pain, and sleep disorder: 

Glycine transporter inhibiting substances

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Toshima-ku, Japan

Minoru Moriya