반응 #1703171

반응 방정식

sodium carbonate

4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-indole

6-bromo-3-fluoro-1H-indazol-4-amine

water

→

title compound

3-Fluoro-6-(1H-indol-4-yl)-1H-indazol-4-amine

용매

1,4-dioxane

반응 조건

후처리

1. 1
   기타The reaction vessel was sealed
2. 2
   온도After cooling
3. 3
   세척was then eluted with methanol (4 column volumes)
4. 4
   workup.DISSOLUTIONre-dissolved in methanol (3 ml)
5. 5
   여과filtered

실험 절차

To 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-indole (24 mg) and 1,1′-bis(diphenylphosphino)ferrocenedichloropalladium(II) (3 mg) at 20° C. in a microwave vial was added a solution of 6-bromo-3-fluoro-1H-indazol-4-amine (19 mg) in 1,4-dioxane (0.75 ml) followed by water (0.5 ml) and aqueous sodium carbonate (2M, 0.124 ml). The reaction vessel was sealed and heated under microwave irradiation at 150° C. for 15 min. After cooling, the black solution was loaded onto a 500 mg silica cartridge which was then eluted with methanol (4 column volumes). The eluant was blown to dryness, re-dissolved in methanol (3 ml), filtered and blown to dryness to give the title compound (67 mg) as a brown film.

출처