反应 #313509

反应方程式

ethyl (2E)-3-(6-{(tert-butoxycarbonyl)[(3R)-3-pyrrolidinyl]amino}-3-pyridyl)acrylate dihydrochloride

[4-(bromomethyl)phenyl](phenyl)methanone

THF

→

ethyl (2E)-3-{6-[[(3R)-1-(4-benzoylbenzyl)-3-pyrrolidinyl](tert-butoxycarbonyl)amino]-3-pyridyl}acrylate

收率 77.6%

溶剂

Et3N

反应条件

后处理

1. 1
   其他the reaction mixture was partitioned between ethyl acetate and water
2. 2
   洗涤The organic layer was washed with brine
3. 3
   干燥dried over MgSO4
4. 4
   过滤filtered
5. 5
   其他evaporated in vacuo
6. 6
   其他The residue was purified by column chromatography on silica gel

实验过程

To a mixture of ethyl (2E)-3-(6-{(tert-butoxycarbonyl)[(3R)-3-pyrrolidinyl]amino}-3-pyridyl)acrylate dihydrochloride (150 mg), [4-(bromomethyl)phenyl](phenyl)methanone (143 mg), and THF (3.5 mL) was added Et3N (0.168 mL). After stirring for 2 hours at room temperature, the reaction mixture was partitioned between ethyl acetate and water. The organic layer was washed with brine, dried over MgSO4, filtered, and evaporated in vacuo. The residue was purified by column chromatography on silica gel to give ethyl (2E)-3-{6-[[(3R)-1-(4-benzoylbenzyl)-3-pyrrolidinyl](tert-butoxycarbonyl)amino]-3-pyridyl}acrylate (149 mg).

来源