(4-Fluoro-3-methylphenyl)boronic acid → 2-(3-(4-Fluoro-3-methyl-phenyl)-5-phenyl-(1,2,4)triazol-1-yl)-1-(4-pyrimidin-2-yl-piperazin-1-yl)-ethanone

참여 물질

역할	이름	HCID	투입량
반응물	(4-Fluoro-3-methylphenyl)boronic acid	HCID 2774580	—
반응물	Sodium dicarbonate	HCID 22718997	—
반응물	2-(3-Bromo-5-phenyl-(1,2,4)triazol-1-yl)-1-(4-pyrimidin-2-yl-piperazin-1-yl)-ethanone	HCID 86690171	—
촉매	HCID 178418397	HCID 178418397	—
용매	1,4-Dioxane	HCID 31275	—
생성물	2-(3-(4-Fluoro-3-methyl-phenyl)-5-phenyl-(1,2,4)triazol-1-yl)-1-(4-pyrimidin-2-yl-piperazin-1-yl)-ethanone	HCID 71612649	30%

반응 조건

온도	120 °C

반응 단계

15 mg tetrakis(triphenylphosphine)palladium(0) was added to 100 mg 2-(3-bromo-5-phenyl-(1,2,4)triazol-1-yl)-1-(4-pyrimidin-2-yl-piperazin-1-yl)-ethanone, 500 μL 2 mol/L aqueous sodiumdicarbonate solution and 43 mg 4-fluoro-3-methylphenylboronic acid in 10 mL dioxane under nitrogen. The reaction was stirred over night at 120° C. The reaction was filltered and evaporated. The residue was purified by HPLC to give 32 mg of the desired product.

출처 및 근거

DOI	10.6084/m9.figshare.5104873.v1
특허 번호	US08889677B2
출처 데이터셋	uspto-grants-2014_11
ORD ID	ord-84aea2a5210d410c990142fca04841a1
출처 메모	uspto-grants-2014_11