反応 #1563932

反応方程式

tert-Butyl 2-oxopyrrolidine-1-carboxylate

Isopropyl magnesium chloride

2-bromo-1,4-difluorobenzene

→

title compound

収率 83.3%

tert-butyl 5-(2,5-difluorophenyl)-2,3-dihydro-1H-pyrrole-1-carboxylate

収率 83.3%

溶媒

THF

THF

THF

反応条件

後処理

1. 1
   workup.STIRRINGstirring
2. 2
   workup.WAITwas continued at 10° C. for 2 h
3. 3
   その他Reaction mixture
4. 4
   その他was quenched with saturated NH4Cl solution
5. 5
   抽出extracted with EtOAc
6. 6
   乾燥dried over anhydrous sodium sulphate
7. 7
   濃縮concentrated under reduced pressure

実験手順

2.0 M Isopropyl magnesium chloride solution in THF (163 mL, 324.3 mmol) was added to a solution of 2-bromo-1,4-difluorobenzene (62.5 g, 324.3 mmol) in THF (350 mL) at −40° C. and stirring was continued at 5° C. for 1 h. tert-Butyl 2-oxopyrrolidine-1-carboxylate (Step-1) (73 g, 392 mmol) in THF (150 mL) was added dropwise to above reaction mixture at −40° C. and stirring was continued at 10° C. for 2 h. Reaction mixture was quenched with saturated NH4Cl solution, extracted with EtOAc, dried over anhydrous sodium sulphate and concentrated under reduced pressure to afford 76 g of the title compound.

出典