تفاعل #84051

معادلة التفاعل

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

المذيبات

DMF

ظروف التفاعل

المعالجة

1. 1
   ترشيحThe resin is filtered off with suction
2. 2
   غسيلwashed twice each with 20 ml each of DMF, THF and DCM
3. 3
   أخرىdried under high vacuum

الإجراء التجريبي

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.

المصدر