Fuji Yakuhin Co., Ltd

Sachiho Miyata

Junichiro Uda

Osamu Nagata

Yoshiyuki Iwabuchi

Koji Matsumoto

Takahiro Sato

Tsutomu Inoue

Tadashi Inoue

Hiroyuki Nakano

Seiichi Kobashi

Naoki Ashizawa

Takashi Iwanaga

Takamitsu Kandou

Tetsuya Taniguchi

To provide an industrially useful method for producing pharmaceutically useful 4-[5-(pyridin-4-yl)-1H-1,2,4-triazol-3-yl]pyridine-2-carbonitrile, and an intermediate for producing the compound. The method for producing compound represented by formula (1) is represented by the following reaction scheme, and the intermediate is represented by the following formula (4). 

Method for producing 4-[5-(pyridin-4-yl)-1H-1,2,4-triazol-3-yl]pyridine-2-carbonitrile, and intermediate thereof

To provide crystal polymorphs of 4-[5-(pyridin-4-yl)-1H-1,2,4-triazol-3-yl]pyridine-2-carbonitrile, which is a useful pharmaceutical, and a production method therefor. Through purification of a corresponding salt, recrystallization, or storage under humidified conditions, three different crystal forms; i.e., crystalline polymorphs of 4-[5-(pyridin-4-yl)-1H-1,2,4-triazol-3-yl]pyridine-2-carbonitrile are produced.

4-[5-(pyridin-4-yl)-1H-1,2,4-triazol-3-yl]pyridine-2-carbonitrile crystalline polymorph and production method therefor

Disclosed are a novel compound and a pharmaceutical product, each having a remarkable uricosuric effect. Specifically disclosed are: a novel phenol derivative represented by general formula (1) that is shown in FIG.; a pharmaceutically acceptable salt thereof; a hydrate of the derivative or the salt; and a solvate of the derivative or the salt. (In the formula, Rand Rmay be the same or different and each represents a lower alkyl group, a lower alkenyl group, a lower alkynyl group, a lower alkoxy group, a haloalkyl group, a haloalkoxy group, an alkylsulfanyl group, an alkylsulfinyl group, an alkylsulfonyl group, a lower alkyl-substituted carbamoyl group, a saturated nitrogen-containing heterocyclic N-carbonyl group, a halogen atom, a cyano group or a hydrogen atom; Rrepresents a lower alkyl group, a haloalkyl group, a halogen atom, a hydroxy group or a hydrogen atom; and X represents a sulfur atom, an &#x2014;S(&#x2550;O)&#x2014; group or an &#x2014;S(&#x2550;O)&#x2014; group.)

Phenol derivative

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Saitama, Japan

Sachiho Miyata