반응 #164222

반응 방정식

[(4-fluoro-phenyl)-methyl-amino]-phenyl-acetic acid (R)-(1-aza-bicyclo[2.2.2]oct-3-yl)ester

2-chloro-1-(thiophen-2-yl)ethanone

→

title compound

수율 84.0%

(R)-3-{2-[(4-fluoro-phenyl)-methyl-amino]-2-phenyl-acetoxy}-1-(2-oxo-2-thiophen-2-yl-ethyl)-1-azonia-bicyclo[2.2.2]octane chloride

수율 84.0%

용매

ethyl acetate

반응 조건

후처리

1. 1
   기타The suspension is evaporated
2. 2
   기타the residue is triturated with Et2O (8 mL)
3. 3
   여과The solid is filtered on a buckner funnel
4. 4
   workup.DISSOLUTIONthe sticky solid is dissolved in DCM
5. 5
   기타The solution is evaporated

실험 절차

To a solution of [(4-fluoro-phenyl)-methyl-amino]-phenyl-acetic acid (R)-(1-aza-bicyclo[2.2.2]oct-3-yl)ester (C120) (100 mg, 0.27 mmol) in ethyl acetate (2.7 mL), is added 2-chloro-1-(thiophen-2-yl)ethanone (48.0 mg, 0.30 mmol). The reaction is stirred at RT for 3.5 days. The suspension is evaporated and the residue is triturated with Et2O (8 mL). The solid is filtered on a buckner funnel and the sticky solid is dissolved in DCM. The solution is evaporated giving the title compound as a pale yellow solid (120 mg, 84% yield, chloride salt, mixture of diastereoisomers).

출처