反応 #84051

反応方程式

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

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

溶媒

DMF

反応条件

後処理

1. 1
   ろ過The resin is filtered off with suction
2. 2
   洗浄washed twice each with 20 ml each of DMF, THF and DCM
3. 3
   その他dried under high vacuum

実験手順

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.

出典