Mitsubishi Tanabe Pharma Corporation

Takanori Higashijima

Yoshinori Nakamura

Hitoshi Kubota

Norimitsu Hayashi

Kozo Oka

Yoshikazu Mori

Masaki Okamoto

Akira Sakuragi

Muneki Kishida

Yasuo Yamamoto

Takeshi Hamada

Shigeki Igarashi

The present invention relates to a method for preparing an optically active cyclic alcohol compound represented by general formula [I]: [wherein R represents a hydrogen atom or a protecting group for amino group, and * represents an asymmetric carbon atom.] [wherein R has the same meaning as defined above.]

Optically active cyclic alcohol compound and method for preparing the same

Optically active cyclic alcohol compound

The present invention is to provide a process for preparing optically active tetrahydroquinoline derivatives which can be used for the treatment and/or prevention of diseases such as arteriosclerotic diseases, dyslipidemia and the like, and a process for preparing synthetic intermediates thereof. Specifically, (2R,4S)-2-ethyl-6-trifluoromethyl-1,2,3,4-tetrahydroquinolin-4-ylamine or a salt thereof is prepared with fewer steps without using an optical resolution, and the optically active tetrahydroquinoline derivatives are obtained from the amine compound.

Process for preparing tetrahydroquinoline derivatives

The present invention relates to a compound of the general formula (1): wherein, Y is a methylene group, and the like; A is an optionally substituted heterocyclic group, and the like; B is an optionally substituted phenyl group, and the like; Ris an optionally substituted alkyl group, and the like; and Ris an optionally substituted amino group, and the like; or a pharmaceutically acceptable derivative thereof, which has an inhibitory activity against cholesteryl ester transfer protein (CETP), thereby being useful for prophylaxis and/or treatment of arteriosclerotic diseases, hyperlipemia or dyslipidemia, and the like.

Trisubstituted amine compound

A novel compound of the formula (I): wherein Ris alkoxycarbonyl or the like, Ris alkyl or the like; Ris hydrogen or the like; Ris alkylene or the like; Ris optionally substituted heterocyclic group; R, R, and Rare independently hydrogen; alkyl, alkoxy, or the like; Ris optionally substituted aromatic ring, or the like; or a pharmaceutically acceptable salt thereof, which has an inhibitory activity against cholesteryl ester transfer protein (CETP).

Tetrahydronaphthyridine derivatives and a process for preparing the same

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Osaka, Japan

Takanori Higashijima