Sumitomo Dainippon Pharma Co., Ltd.

Dainippon Sumitomo Pharma Co., Ltd.

Sumitomo Pharma Co., Ltd.

Hiroto Tatamidani

Satoshi Suzuki

Kazuki Hashimoto

Toshikazu Yagi

Yoko Takahashi

Shinjiro Tsuyumine

Naoya Kinomura

Satoshi Nojima

Masahiro Takamura

Keisuke Kakiguchi

Megumi Maruyama

The present invention provides a method in which when using (+)-dibenzoyl-D-tartaric acid to optically divide (±)-1-methyl-4-(2,4,6-trimethoxyphenyl)-3-piperidinone, an ether-based solvent is added and an extremely high yield of (R)-1-methyl-4-(2,4,6-trimethoxyphenyl)-3-piperidinone (+)-dibenzoyl-D-tartrate is thereby obtained, a slurry thereof is treated with a base, a 'three-dimensionally bulky reducing agent' is subsequently used, and cis-(−)-flocinopiperidol is thereby produced with surprisingly high selectivity.

Method for producing cis-(-)-flocino piperidol

The invention addresses the problem of providing a method for producing 2-acetyl-4H,9H-naphtho[2,3-b]furan-4,9-dione that is suited to industrial production. The invention provides a method for producing 2-acetyl-4H,9H-naphtho[2,3-b]furan-4,9-dione by reacting 3-bromo-3-buten-2-one and 2-hydroxy-1,4-naphthoquinone in the presence of a solvent, then obtaining crystals of 2-acetyl-4H,9H-naphtho[2,3-b]furan-4,9-dione by adding an alcohol-based solvent and/or water to the reaction system, and treating the crystals by using a specific adsorbent in the presence of a solvent.

Method for producing 2-acetyl-4H,9H-naphtho[2,3-b]furan-4,9-dione

Method for producing 2-acetyl-4H,9H-naphtho[2,3-B]furan-4,9-dione

The present invention provides compounds which show high effectiveness against positive symptoms, negative symptoms and cognitive dysfunction in schizophrenia and reduce conventional side-effect risks as well as have remarkable effects for central neurological diseases associated with cognitive dysfunction other than schizophrenia. N-Acyl cyclic amine derivatives of formula (1): wherein Arand Arare aryl or heteroaryl; V is nitrogen, or CR; Wis a single bond, &#x2014;C(O)&#x2014;, etc.; Wis C-alkylene; Wis a single bond, methylene, &#x2014;NH&#x2014;, &#x2014;CR&#x2550;CR&#x2014;, etc.; Ring Q is a group of formula (a) in which n is 0 or 1; m is 0 to 2; k is 1 to 3; Z is a single bond, methylene, oxygen, etc.; R, Rand Rare each, same or different, hydrogen, hydroxyl, halogen, cyano, Calkyl, etc.; or pharmaceutically acceptable salts thereof are provided. 

N-acyl cyclic amine derivative or pharmaceutically acceptable salt thereof

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Osaka, Japan

Hiroto Tatamidani