Daiichi Sankyo Company, Limited

Daiichi Pharmaceutical Co., Ltd.

Tsutomu Yagi

Koji Sato

Akihiro Imura

Kouji Sato

Hiroshi Nagasawa

Yasuo Kitani

Yoshihiro Takayanagi

Keiji Nakayama

Tomoyuki Nagai

Yukinari Kobayashi

Mikihiro Itoh

Katsuhiko Okano

Yutaka Kitagawa

Yuichiro Tani

Hiroshi Maruoka

Seiichi Imajo

Taisaku Tanaka

Tsuyoshi Muto

Yoshiaki Tomimori

Kenji Sakuratani

Kazuo Kubota

Kotaro Kawanami

Shigeru Ichikawa

Yoshihiro Takyanagi

The present invention provides a method for producing a 1-biphenylmethylimidazole compound having superior angiotensin II receptor antagonistic activity, or an intermediate thereof. The present invention provides a method for producing a compound having the formula (5) (R, R: H, an alkyl group) by oxidizing a compound having the formula (1) (R: H, an alkyl group) using an oxidizing agent in the presence of a radical initiation reagent, and then reacting with an ammonia-generating reagent and a compound having the formula RCHO(R: H, an alkyl group) or a compound having the formula RC(OR)(R: H, an alkyl group; R: an alkyl group). 

Method for producing 1-biphenylmethylimidazole compound

The invention is directed to a process for producing intermediates of a compound which exhibits an activated blood coagulation factor Xa inhibitory action and which is a useful preventive and a therapeutic agent for thrombotic diseases. The intermediate production process is represented by the following reaction scheme. 

Optically active diamine derivative and process for producing the same

5-Methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxylic acid of formula (5) or a salt thereof,   

Process for producing 5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxylic acid

A 7-membered heterocyclic compound having the formula (I), or its salt, or a solvate thereof with a chymase inhibitory action and useful for the prevention or treatment of various diseases, in which chymase is involved: a method for producing the same, and a pharmaceutical composition useful for the prevention or treatment of diseases, in which chymase is involved, including the compound of having the formula (I), or its pharmaceutically acceptable salt, or a solvate thereof are provided.

7-membered ring compound and method of production and pharmaceutical application thereof

5-Methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine of formula (6) or a salt thereof, is prepared by reacting 2-amino-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine of formula (2) or a salt thereof, with an alkali metal nitrite in the presence of a reducing agent in an aqueous solution of an acidic compound.

5-Methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxylic acid of formula (5) or a salt thereof, [F14] is prepared by reacting a compound of formula (6) or a salt thereof, with a trihalogenoacetyl halide in the presence of a base, followed by hydrolysis.

Process for producing 5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]Pyridine-2-carboxylic acid

The present invention provides processes for producing a compound (5) based on the following reaction scheme. 

Process for producing thiazole derivative

Treatment of a lactic acid ester derivative with an enzyme or the like, which has asymmetric ester-hydrolyzing ability, can specifically hydrolyze the ester moiety of an isomer existing as the pair to the racemic derivative. Use of the compound obtained by this hydrolysis makes it possible to produce an optically active propoxyaniline derivative by a shorter process than the conventional art 

Process for preparation of optically active propoxyaniline derivatives

Processes for producing antibacterial agents and intermediates useful in producing antibacterial agents are provided and include producing compound (VI-a) in accordance with the following reaction schema, as well as production intermediates thereof 

Process for producing benzoxazine derivative and production intermediate thereof

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 

Method for producing 2-azetidinone derivative

Processes for producing antibacterial agents and intermediates useful in producing antibacterial agents are provided and include producing compound (VI-a) in accordance with the following reaction schema, as well as production intermediates thereof.

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Tokyo, Japan

Tsutomu Yagi