Daiichi Sankyo Company, Limited

Daiichi Pharmaceutical Co., Ltd.

Yutaka Kitagawa

Makoto Muto

Yuichiro Tani

Toshiaki Jyono

Makoto Imai

Masao Fujita

Tatsuya Nakamura

Hitoshi Sato

Yoshitaka Nakamura

Tatsuya Yamaguchi

Shigeru Noguchi

Takahiro Aoki

Tsutomu Yagi

Tsuyoshi Ueda

Manabu Miura

Akihiro Imura

Kouji Sato

Masakazu Wakayama

Shinji Matuura

Kazutoshi Ukai

Takafumi Kitawaki

Kohei Sakanishi

Eiji Numagami

Yukito Furuya

Tadahiro Takeda

Kei Kurahashi

Yohei Yamane

Fumikatsu Kondo

Takashi Kouko

Shigeru Ichikawa

Ayako Saito

Takumi Nakajima

Crystals of the compound represented by formula (1), a method for the production thereof, and a method for producing an antibody-drug conjugate using the crystals.

Method for producing antibody-drug conjugate

An object of the present invention is to provide an optically active bicyclic &#x3b3;-amino acid derivative in a high purity. The object can be attained by a mixture of compounds represented by the general formulas (I) and (I'), or a method for producing a compound represented by the general formula (VII) or a salt thereof via the compound (I): wherein Rand Reach represent a C1-6 alkyl group or the like; and Rrepresents a cyano group or the like, 

Preparation method for optically active bicyclic gamma-amino acid compound

The invention provides an industrial method for producing a spiroaminopyrrolidone derivative, which is an intermediate for producing a quinolone antibacterial agent.

Method for producing asymmetric tetrasubstituted carbon atom-containing compound

Methods for producing compounds having activity as an &#x3b1;&#x3b4; ligand are provided.

Method for producing bicyclic &#x3b3;-amino acid derivative

The invention provides an industrial method for producing a spiroaminopyrrolidone derivative, which is an intermediate for producing a quinolone antibacterial agent. Specifically, the invention provides a method for producing a compound of formula (2): wherein n is an integer of 2 to 5; Ris a (substituted) alkyl group or a (substituted) aryl group; and Rrepresents a (substituted) alkoxycarbonyl group, a (substituted) aralkyloxycarbonyl group, a (substituted) aliphatic acyl group, or a (substituted) aromatic acyl group).

A process for producing an optically active compound represented by formula () or a salt thereof:  

Intermediates for the production of optically active cyclopropylamine derivatives and process for the production of the intermediates

The invention provides an industrial method for producing a spiroaminopyrrolidone derivative, which is an intermediate for producing a quinolone antibacterial agent. The invention provides a method for producing a compound represented by formula (2): (wherein n is an integer of 2 to 5; Rrepresents a (substituted) alkyl group or a (substituted) aryl group; and Rrepresents a (substituted) alkoxycarbonyl group, a (substituted) aralkyloxycarbonyl group, a (substituted) aliphatic acyl group, or a (substituted) aromatic acyl group), which includes treating a compound represented by formula (1): (wherein n, R, and Rare the same as defined above; and Rrepresents a hydrogen atom, a (substituted) alkyl group, or a (substituted) aralkyl group) under a hydrogen gas atmosphere in the presence of a metallic catalyst.

Provision of a commercially advantageous method for producing an intermediate which is important for producing the antibacterial and which has a mother nucleus common to the antibacterial, and intermediates produced by such method. A method for producing a compound represented by formula (VI): which comprises the steps of treating a compound represented by formula (IV): with a base in the presence of a base to produce a compound represented by formula (V): and hydrolyzing this compound;a compound represented by formula (II): a compound represented by formula (Ia): a compound represented by formula (V): and a compound represented by formula (VI). 

Intermediates and process for the production of optically active quinolonecarboxylic acid derivatives

Provided are a technique for position-selectively introducing an amino group into a difluorobenzoic acid, a novel process for producing a quinolonecarboxylic acid derivative serving as an antibacterial agent, and intermediates in the production. The process comprises treating a compound represented by formula (6): with a base in a water-containing solvent. The intermediates are represented by formula (6): 

Method of selectively introducing amino substituent

A process for producing an optically active compound represented by formula (4), or a salt thereof, wherein Rrepresents a protecting group.

A process for producing a compound represented by the following formula (II) which comprises treating a compound represented by the following formula (I) (wherein R, Rand Rrepresent each a specific substituent) with an enzyme capable of asymmetrically hydrolyzing an ester and the novel compound (II). The process of the present invention makes it possible to easily obtain an optically active 2-azetidinone derivative in a large amount at a low cost 

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Edogawa-ku, Japan

Yutaka Kitagawa