反応 #495201

反応方程式

(S)-3-(6-(Methylsulfonyl)pyridin-3-ylamino)-1-(piperidin-4-yl)pyrrolidin-2-one

2,5-dichloropyrazine

DIEA

→

(S)-1-(1-(5-chloropyrazin-2-yl)piperidin-4-yl)-3-(6-(methylsulfonyl)pyridin-3-ylamino)pyrrolidin-2-one

収率 30.5%

溶媒

NMP

反応条件

後処理

1. 1
   温度cooled to ambient temperature
2. 2
   その他The reaction mixture was partitioned between EtOAc (40 mL) and H2O (20 mL)
3. 3
   ろ過The mixture was filtered through a 0.45 μm nylon membrane
4. 4
   洗浄the solids were washed with EtOAc
5. 5
   その他dried under high vacuum

実験手順

(S)-3-(6-(Methylsulfonyl)pyridin-3-ylamino)-1-(piperidin-4-yl)pyrrolidin-2-one (0.076 g, 0.22 mmol) and 2,5-dichloropyrazine (0.054 g, 0.36 mmol) were dissolved in NMP (0.45 mL) and treated with DIEA (0.098 mL, 0.56 mmol). The mixture was stirred at 80° C. overnight and then cooled to ambient temperature. The reaction mixture was partitioned between EtOAc (40 mL) and H2O (20 mL). The mixture was filtered through a 0.45 μm nylon membrane and the solids were washed with EtOAc and then dried under high vacuum to provide (S)-1-(1-(5-chloropyrazin-2-yl)piperidin-4-yl)-3-(6-(methylsulfonyl)pyridin-3-ylamino)pyrrolidin-2-one (0.030 g, 0.067 mmol, 30%).

出典