Benzimidazole → 4-(1H-Benzimidazol-2-yl)-N-(1,3-thiazol-2-yl)benzene-1-sulfonamide

Temperatur

150 °C

Benzimidazole (0.313 mmol) and MgO (0.376 mmol) was stirred in 1,4-dioxane (2 mL) for 10 min. at room temp. To the solution, copper iodide (0.627 mmol), palladium acetate (0.016 mmol), triphenylphosphine (0.062 mmol), and 4-bromo-N-thiazol-2-yl-benzenesulfonamide (0.313 mmol) were added. The reaction was sealed and heated to 150° C. After 7 h the reaction was cooled to 120° C. and stirred overnight. The reaction was cooled to room temperature and diluted with acetone. The solution was filtered through Celite and concentrated in vacuo. The crude was purified by reverse phase chromatography to yield 4-(1H-benzoimidazol-2-yl)-N-thiazol-2-yl-benzenesulfonamide (0.007 mmol).

1. customThe reaction was sealed
2. temperatureAfter 7 h the reaction was cooled to 120° C.
3. temperatureThe reaction was cooled to room temperature
4. filtrationThe solution was filtered through Celite
5. concentrationconcentrated in vacuo
6. customThe crude was purified by reverse phase chromatography

ORD-Eintrag

ord-11b19ce5401e465389a45aed940ef3c2

Quelldatensatz

uspto-grants-2009_11

DOI

10.6084/m9.figshare.5104873.v1

Patentnummer

US07615569B2