Reaktion #605619

Reaktionsgleichung

title compound

5-bromo-7-methyl-[1,2,4]triazolo[4,3-a]pyrazin-8-one

K3PO4

N2

N-[4-(2,4-difluorophenoxy)-3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl]ethanesulfonamide

→

title compound

Ausbeute 49.3%

N-[4-(2,4-difluorophenoxy)-3-(7-methyl-8-oxo-[1,2,4]triazolo[4,3-a]pyrazin-5-yl)phenyl]ethanesulfonamide

Ausbeute 49.3%

Lösungsmittel

dioxane

H2O

Reaktionsbedingungen

Aufarbeitung

1. 1
   Sonstigepurged
2. 2
   Sonstigemicrowaved at 70° C. for 2 h

Vorschrift

The title compound of Example 235, step 2 (40 mg, 0.175 mmol), N-[4-(2,4-difluorophenoxy)-3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl]ethanesulfonamide (77 mg, 0.175 mmol), K3PO4 (93 mg, 0.438 mmol) and Pd(dppf)Cl2 (13 mg, 0.018 mmol) in dioxane (2 mL) and H2O (1 mL) was N2 purged and microwaved at 70° C. for 2 h. Preparative HPLC gave the title compound (38.75 mg, yield: 49.3%) as an off-white solid. 1H NMR (CDCl3, 400 MHz): δ 8.60 (s, 1H), 7.64 (d, J=2.8 Hz, 1H), 7.45 (dd, J1=8.8 Hz, J2=2.8 Hz, 1H), 7.10-7.05 (m, 1H), 6.99-6.88 (m, 3H), 6.74 (d, J=8.8 Hz, 1H), 3.67 (s, 3H), 3.18 (q, J=7.2 Hz, 2H), 1.40 (t, J=7.2 Hz, 3H). LCMS: 462.0 (M+H)+

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