تفاعل #1764382

معادلة التفاعل

2-Ethanesulfonyl-5-iodo-pyridine

(4-carboxy-3-fluorophenyl)boronic acid

sodium carbonate

→

4-(6-Ethanesulfonyl-pyridin-3-yl)-2-fluoro-benzoic acid

المذيبات

dioxane

ظروف التفاعل

المعالجة

1. 1
   درجة الحرارةHeat
2. 2
   أخرىthe reaction
3. 3
   درجة الحرارةto reflux for 4 hours
4. 4
   أخرىAfter this time, remove the
5. 5
   درجة الحرارةheat
6. 6
   تركيزconcentrate in vacuo
7. 7
   غسيلWash with dichloromethane
8. 8
   استخلاصwhile extracting with water
9. 9
   استخلاصextract with 10% isopropanol/dichloromethane four times
10. 10
    تجفيفCombine the organics, dry with sodium sulfate
11. 11
    أخرىdecant
12. 12
    تركيزconcentrate in vacuo

الإجراء التجريبي

Procedure VV: To a stirring solution of 2-Ethanesulfonyl-5-iodo-pyridine (1.0 mmol) and (4-carboxy-3-fluorophenyl)boronic acid (1.3 mmol) in dioxane (0.1M), add dichloro[1,1′-bis(diphenylphosphino)ferrocene]palladium dichloromethane complex (0.03 mmol) and 2M aqueous sodium carbonate (3.0 mmol). Heat the reaction to reflux for 4 hours. After this time, remove the heat and concentrate in vacuo. Wash with dichloromethane while extracting with water. Acidify the aqueous layer with 1N hydrochloric acid and extract with 10% isopropanol/dichloromethane four times. Combine the organics, dry with sodium sulfate, decant and concentrate in vacuo. MS (m/e): 310.3 (M+1)

المصدر