Taisho Pharmaceutical Co., Ltd.

Hideaki Tabuse

Norikazu Otake

Ryo Suzuki

Hiroshi Ohta

Tsuyoshi Shibata

Hiroki Urabe

Shoichi Kuroda

Yohei Matsuda

Yohei Kobashi

Yasunobu Ushiki

Fumito Uneuchi

Kenichi Kawabe

Daisuke Matsuda

Minoru Moriya

Aya Futamura

Nobutaka Hattori

Koreaki Imura

Eiji Munetomo

Sumi Chonan

Ryo Kinoshita

Rie Shimono

Takaaki Matsubara

Tomokazu Tamaoki

Provided is a novel process for producing a (2S)-2-[(1H-pyrazol-1-yl)methyl]-1,3-oxazinane derivative. More specifically, provided is a process for producing a (2S)-2-[(1H-pyrazol-1-yl)methyl]-1,3-oxazinane derivative represented by formula (1): 

Method for producing (2S)-2-[(1H-pyrazol-1-yl)methyl]-1,3-oxazinane derivative

A novel process for producing optically active 2-(2-fluorobiphenyl-4-yl)propanoic acid is disclosed. This production process is characterized in that a compound of formula [1] is reacted with magnesium and so forth to prepare an organometallic reagent, which is reacted with a compound of formula [2] in the presence of a catalytic amount of a nickel compound and a catalytic amount of an optically active compound of formula [3] to obtain a compound represented by formula [4] which is subsequently converted to a compound represented by formula [5] or a pharmaceutically acceptable salt thereof. 

Method for producing optically active 2-(2-fluorobiphenyl-4-yl) propanoic acid

The present invention provides a compound represented by the following formula [1] or a pharmaceutically acceptable salt thereof which has an excellent NHE3 inhibitory effect:A-Y&#x2003;&#x2003;[1]wherein  

Phenyl tetrahydroisoquinoline compound substituted with heteroaryl

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Tokyo, Japan

Hideaki Tabuse