Kaken Pharmaceutical Company, Ltd.

Takuya Yamada

Noriyuki Kamei

Yoshitake Sumikawa

Shingo Todo

Shota Tokuoka

Daigo Kamimura

Nobuo Ishiyama

Mitsuo Mimura

Masahito Watanabe

General formula (I): The present invention pertains to: a pyridone derivate or a salt thereof represented by general formula (I); or a medicine containing the pyridone derivative or salt thereof as an active ingredient. [In the formula, ring A, R, R, Rand Rare specific groups.] 

Pyridone derivative, pharmaceutical containing the same and methods of use thereof

Pyridone derivative and pharmaceutical containing same

An object is to provide a process for producing the compound of formula 1 in higher yield by the ring-opening addition reaction of epoxytriazole with amine under mild conditions without using a large excess of 4-methylenepiperidine. The process for producing (2R,3R)-2-(2,4-difluorophenyl)-3-(4-methylenepiperidin-1-yl)-1-(1H-1,2,4-triazol-1-yl)butan-2-ol or an acid addition salt thereof comprises reacting (2R,3S)-2-(2,4-difluorophenyl)-3-methyl-2-[(1H-1,2,4-triazol-1-yl)methyl]oxirane with an acid addition salt of 4-methylenepiperidine in a reaction solvent in the presence of a hydroxide of an alkali metal or an alkaline earth metal selected from the group consisting of lithium, sodium, calcium, and strontium, or a hydrate thereof.

Process for producing 1-triazole-2-butanol derivatives

Growing community of inventors

Kyoto, Japan

Takuya Yamada