Mitsubishi Tanabe Pharma Corporation

Takeshi Hamada

Toru Iijima

Hidenori Akatsuka

Kenichi Toyama

Tomoyuki Okabe

Atsushi Moroda

Kaori Tomikawa

Yoshihiro Sugiura

Yukie Okamoto

Yoshinori Nakamura

Hitoshi Kubota

Norimitsu Hayashi

Masaki Okamoto

Yoshikazu Mori

Takanori Higashijima

Akira Sakuragi

The present invention provides an industrially advantageous method for producing a 1,4-benzoxazine compound useful as a medicine while avoiding safety and health risks. Specifically, the present invention provides a method for producing a 1,4-benzoxazine compound [A], which comprises the three steps in the following scheme, namely, a step of converting the amino group at 7-position in a compound [a] into a dimesylamino group, a step of coupling a compound [b] with a boronic acid compound, and a step of converting the 7-position in a compound [c] into a monomesylamino group.  In the above scheme, Ms is a methanesulfonyl group, and each of R' and R&#x2033; is a hydrogen atom etc.

Method for producing 1,4-benzoxazine 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

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Osaka, Japan

Takeshi Hamada