Taisho Pharmaceutical Co., Ltd.

Other

Sagami Chemical Research Center

Nihon Nohyaku Co., Ltd.

Cogstate, Ltd.

Kazuyuki Tomisawa

Atsuro Nakazato

Toshihito Kumagai

Shigeyuki Chaki

Masanori Yoshida

Masashi Nagamine

Taketoshi Okubo

Makoto Gotoh

Kazunari Sakagami

Kazuya Kameo

Toru Matsunaga

Kaoru Sota

Tomomi Ota

Shiuji Saito

Kenji Yamamoto

Toshio Nakamura

Minoru Taguchi

Yoshimoto Nakashima

Koichiro Harada

Izumi Aibe

Misa Nakanishi

Hideo Tanaka

Jiro Sawada

Chihiro Yokoo

Takeo Taguchi

Shigeru Okuyama

Kikuo Sugimoto

Masami Nemoto

Haruo Shimamura

Fumio Urushizaki

Hironaka Aihara

Takeo Kobori

Yasuhide Tachi

Tomomichi Yoshida

Kenichi Goda

Michio Kurachi

Kazumasa Ogino

Tuguchika Yoshida

Kuniaki Kondoh

Hisanako Ito

Kaoru Sata

Dai Tatsuta

Hisanaka Ito

The present invention provides a safer method for production of a cis-4-fluoro-L-proline derivative under milder conditions and in good yield to give a product of high purity on an industrial scale at low cost. Namely, the present invention provides a method for producing a cis-4-fluoro-L-proline derivative, which comprises reacting a trans-4-hydroxy-L-proline derivative of the following Formula [I]: (wherein Rrepresents a protecting group for an &#x3b1;-amino group, and Rrepresents a protecting group for a carboxyl group) with N,N-diethyl-N-(1,1,2,3,3,3-hexafluoropropyl)amine in the presence of a hydrogen fluoride-scavenger.

Method for production of cis-4-fluoro-L-proline derivatives

Carbamoyl tetrahydropyridine derivatives represented by the formula:[in the formula, Rand Rare identical or different, and each represents a hydrogen atom, a C-Calkyl group, or the like; Y&#x2014;Yrepresents (R)C&#x2550;C(R), (R)C&#x2550;N, N&#x2550;N, (R) N&#x2014;CO, or N&#x2550;C(R); X, X, and Xare identical or different, and each represents a hydrogen atom, a halogen atom, or the like; R, R, R, and Rare identical or different, and each represents a hydrogen atom or an alkyl group; Rrepresents a hydrogen atom, a C-Calkyl group, or the like; and Rrepresents a hydrogen atom or a carbamoyl group] or a pharmaceutically acceptable salt thereof, and intermediates for the preparation thereof are provided. The derivatives described above are effective for diseases which are believed to involve CRF.

Carbamoyl tetrahydropyridine derivatives

Arylpiperidine derivatives and use thereof

Carboxylic acid derivatives and process for producing the same

Carboxylic acid derivatives and process for producing same

Heterocycle substituted aryloxyaniline derivatives and their use as MDR ligands

Intermediates and process for producing fluorine-containing amino acid compound by using the same

1,2-dihydro-2-oxoquinoline derivatives

The present invention provides fluorobicyclo&lsqb;3.1.0&rsqb;hexane derivatives represented by the formula

6-fluorobicyclo&lsqb;3.1.0&rsqb;hexane derivatives

An aryloxyaniline derivative represented by the formula:

Aryloxyaniline derivatives

A 1,2-dihydro-2-oxoquinoline derivative represented by the formula:

1,2-Dihydro-2-oxoquinoline derivatives

Fluorine-containing amino acid derivatives represented general formula (I), pharmaceutically acceptable salts thereof or hydrates of the same, wherein X,represents hydrogen or fluorine; and R,and R,are the same or different and each represents hydrogen or lower C,alkyl. These compounds are useful as drugs, in particular, group 2 metabotropic glutamate receptor agonists for treating and preventing psychiatric disorders such as schizophrenia, anxiety and associated diseases, depression, bipolar disturbance and epilepsy, and neurological diseases such as drug addiction, cognition disorder, Alzheimer's disease, Huntington's chorea, Parkinson's disease, motility disturbance associating muscular stiffness, cerebral ischemia, cerebral insufficiency, spinal cord lesion and head disturbance.

Fluorine-containing amino acid derivatives

An aromaheterocyclic derivative represented by the formula:

Heteroaromatic derivatives

Growing community of inventors

Tokyo, Japan

Kazuyuki Tomisawa