Mitsubishi Tanabe Pharma Corporation

Janssen Pharmaceutica Nv

Mitsuhiro Yada

Masanori Hatsuda

Masahiko Yoshinaga

Christopher A Teleha

Rudy Laurent Maria Broeckx

Walter Ferdinand Maria Filliers

Koichi Tanimoto

Patrick Hubert J Nieste

Koji Matsuyama

The present invention provides an industrially advantageous method for producing an optically active naphthalene compound useful as a therapeutic agent for dermatitis or the like. Specifically, the present invention provides a method for producing an optically active naphthalene compound [I], which comprises: a step of reacting a compound [a-1] and a compound [b-1] with each other in the presence of a base and a catalyst that is composed of a Pd compound and a tertiary phosphine ligand (step a); a step of asymmetrically hydrogenating a compound [c-1] in the presence of a hydrogen donor and a complex that is prepared from a ruthenium compound and a chiral ligand, or alternatively in the presence of an optically active oxazaborolidine compound (a CBS catalyst) and a boron hydride compound (step b); and a step of treating a compound [d-1] with a reducing agent (step c). (In the above formulae, Rand Rrepresent the same or different lower alkyl groups; and Xrepresents a halogen atom.). 

Method for producing optically active naphthalene compound

The present invention is directed to a novel process for the preparation of compounds having inhibitory activity against sodium-dependent glucose transporter (SGLT) being present in the intestine or kidney.

Process for the preparation of compounds useful as inhibitors of SGLT

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Sanyoonoda, Japan

Mitsuhiro Yada