Reacción #164222

Ecuación de reacción

[(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

Rendimiento 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

Rendimiento 84.0%

Disolventes

ethyl acetate

Condiciones de reacción

Tratamiento posterior

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

Procedimiento

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).

Fuente