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HRID 43558作成日:2026年10月26日

Lithium Hydroxide → cis(+/-)-2-{3-(Benzyloxy)-4-[(1H-imidazol-2-ylcarbonyl)amino]piperidin-1-yl}-1,3-thiazole-5-carboxylic acid

https://huagongshe.com/reaction/43558

反応式

関与物質

役割名称HCID仕込み量
反応物Lithium HydroxideHCID 3939—
反応物Ethyl cis(+/-)-2-{3-(benzyloxy)-4-[(1H-imidazol-2-ylcarbonyl)amino]piperidin-1-yl}-1,3-thiazole-5-carboxylateHCID 86648573—
溶媒MethanolHCID 887—
溶媒DichloromethaneHCID 6344—
生成物cis(+/-)-2-{3-(Benzyloxy)-4-[(1H-imidazol-2-ylcarbonyl)amino]piperidin-1-yl}-1,3-thiazole-5-carboxylic acidHCID 8664857466%

反応条件

温度70 °C

反応手順

Ethyl cis(±)-2-{3-(benzyloxy)-4-[(1H-imidazol-2-ylcarbonyl)amino]piperidin-1-yl}-1,3-thiazole-5-carboxylate obtained in Example (90f) (0.25 g, 0.55 mmol) was dissolved in methanol (5 mL) and dichloromethane (1 mL). A 2 N aqueous lithium hydroxide solution (5 mL, 10 mmol) was added, and the mixture was stirred at 70° C. for 20 minutes. The organic solvent was evaporated under reduced pressure, and 1 N hydrochloric acid was added until the pH of the solution was about 4. Purification by reverse phase chromatography (elution solvent: acetonitrile/water=1/1, 4/1) gave 0.15 g of the title compound as a white solid (66%).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08536197B2
出典データセットuspto-grants-2013_09
ORD IDord-28c11b907bf24a818479a4c20316c540
出典メモuspto-grants-2013_09