反応 #72206

反応方程式

Ethyl 2-[(3S)-3-{[(4-chloro-5-ethyl-1H-imidazol-2-yl)carbonyl]amino}pyrrolidin-1-yl)-4-methyl-1,3-thiazole-5-carboxylate

lithium hydroxide

Water

→

title compound

収率 77.7%

2-[(3S)-3-{[(4-Chloro-5-ethyl-1H-imidazol-2-yl)carbonyl]amino}pyrrolidin-1-yl)-4-methyl-1,3-thiazole-5-carboxylic acid

収率 77.7%

溶媒

methanol

反応条件

後処理

1. 1
   洗浄the mixture was washed with ethyl acetate
2. 2
   workup.ADDITIONA 1 N aqueous hydrochloric acid solution (5 mL) was added to the aqueous layer
3. 3
   ろ過The precipitated solid was collected by filtration
4. 4
   洗浄washed with water and ethyl acetate

実験手順

Ethyl 2-[(3S)-3-{[(4-chloro-5-ethyl-1H-imidazol-2-yl)carbonyl]amino}pyrrolidin-1-yl)-4-methyl-1,3-thiazole-5-carboxylate obtained in Example (237b) (215 mg, 0.52 mmol) was dissolved in methanol (5 mL). A 2 N aqueous lithium hydroxide solution (2.61 mL, 5.22 mmol) was added, and the mixture was stirred at 40° C. for two hours. Water was added to the reaction solution, and then the mixture was washed with ethyl acetate. A 1 N aqueous hydrochloric acid solution (5 mL) was added to the aqueous layer. The precipitated solid was collected by filtration and washed with water and ethyl acetate to obtain 155 mg of the title compound as a white solid (77%).

出典