反応 #164222

反応方程式

[(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

収率 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

収率 84.0%

溶媒

ethyl acetate

反応条件

後処理

1. 1
   その他The suspension is evaporated
2. 2
   その他the residue is triturated with Et2O (8 mL)
3. 3
   ろ過The solid is filtered on a buckner funnel
4. 4
   workup.DISSOLUTIONthe sticky solid is dissolved in DCM
5. 5
   その他The solution is evaporated

実験手順

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).

出典