Reaktion #1983673

Reaktionsgleichung

polymeric support resin

4-Hydroxy-2,3,5,6-tetrafluorobenzoic Acid

1-azabicyclo[2.2.2]oct-3-ylacetic acid hydrochloride

N,N′-diisopropylcarbodiimide

→

polymer-bound title compound

4-{2-(1-Azabicyclo[2.2.2]oct-3-yl)acetoxy}-2,3,5,6-tetrafluorobenzoic Acid

Lösungsmittel

DMF

Reaktionsbedingungen

Aufarbeitung

1. 1
   FiltrationThe resin is filtered off with suction
2. 2
   Waschenwashed twice each with 20 ml each of DMF, THF and DCM
3. 3
   Sonstigedried under high vacuum

Vorschrift

2 g of the polymeric support resin from Example 8A (loading about 1.36 mmol/g, 2.72 mmol) are suspended in 20 ml of DMF and shaken with 1.23 g (5.98 mmol) of 1-azabicyclo[2.2.2]oct-3-ylacetic acid hydrochloride and 130 mg (1.09 mmol) of DMAP for 10 min. Then 1.06 ml (6.80 mmol) of N,N′-diisopropylcarbodiimide are added, and the mixture is shaken overnight. The resin is filtered off with suction, washed twice each with 20 ml each of DMF, THF and DCM and dried under high vacuum. 2.318 g of the polymer-bound title compound are obtained.

Quelle