4-Cyano-2-fluorophenylboronic acid, pinacol ester synthesis

Yield: 98%

Reaction Conditions:

with (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride;potassium acetate in 1,4-dioxane at 110;Inert atmosphere;

Steps:

1
E2-1 was synthesized by suspending 4-bromo-3-fluorobenzonitrile (CAS 133059-44-6, 1.0 eq.), bis(pinacolato)diboron (CAS 73183-34-3, 1.2 eq.) ), [1,1'-bis(diphenylphosphino)ferrocene]dichloropalladium(II) (Pd(dppf)Cl2, CAS 72287-26-4, 0.026 eq) and potassium acetate (CAS 127-08-2, 3 equiv.) in dry dioxane under nitrogen atmosphere and stirring (1 to 2 hours) at 110 ° C. Then, activated carbon and Celite (kieselgur) were added, and the mixture was stirred at 110 ° C for 20 minutes, followed by high temperature filtration. After concentrating the filtrate under reduced pressure,E2-1 was obtained as a solid, (98% yield).

References:

Si Nora Geembeha;Si Peo-man-syu-te-pan KR2020/21892, 2020, A Location in patent:Paragraph 0557-0558