تفاعل #164222

معادلة التفاعل

[(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

المردود 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

المردود 84.0%

المذيبات

ethyl acetate

ظروف التفاعل

المعالجة

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

الإجراء التجريبي

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).

المصدر