반응 #2294463

반응 방정식

tert-butyl((5-chloro-4-((6-chloro-4-(furan-3-yl)pyridin-3-yl)oxy)-2-fluorophenyl)sulfonyl)(thiazol-4-yl)carbamate

(2-fluoropyridin-3-yl)boronic acid

Na2CO3

→

title compound

수율 72.0%

5-chloro-2-fluoro-4-((2′-fluoro-4-(furan-3-yl)-[2,3′-bipyridin]-5-yl)oxy)-N-(thiazol-4-yl)benzenesulfonamide

수율 72.0%

용매

1,4-dioxane H2O

반응 조건

후처리

1. 1
   workup.ADDITIONwere added
2. 2
   기타1,4-dioxane was removed
3. 3
   농축by concentrating under reduced pressure
4. 4
   추출After extracting with ethyl acetate
5. 5
   workup.ADDITIONthe extract was treated with MgSO4
6. 6
   농축concentrated under reduced pressure
7. 7
   기타The residue was separated by PLC (developing solvent, EA:n-Hex=1:1)

실험 절차

10 mg of tert-butyl((5-chloro-4-((6-chloro-4-(furan-3-yl)pyridin-3-yl)oxy)-2-fluorophenyl)sulfonyl)(thiazol-4-yl)carbamate was dissolved in 1,4-dioxane/H2O=1:1 (0.38 mL), and 3.5 mg of (2-fluoropyridin-3-yl)boronic acid, 0.65 mg (3 mol %) of Pd(PPh3)4 and 5.96 mg of Na2CO3 were added thereto. After reacting with microwave reactor at 120° C. for 5 minutes, 1,4-dioxane was removed by concentrating under reduced pressure. After extracting with ethyl acetate, the extract was treated with MgSO4, and concentrated under reduced pressure. The residue was separated by PLC (developing solvent, EA:n-Hex=1:1) to obtain 6.7 mg (72% yield) of the title compound.

출처