3-Fluoro-4-nitrophenylboronic acid,pinacol ester synthesis
- Product Name:3-Fluoro-4-nitrophenylboronic acid,pinacol ester
- CAS Number:939968-60-2
- Molecular formula:C12H15BFNO4
- Molecular Weight:267.06
321-23-3
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$10.00/1g
73183-34-3
556 suppliers
$6.00/5g
939968-60-2
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$71.00/100mg
Yield: 78.6%
Reaction Conditions:
with (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride;potassium acetate in 1,4-dioxane at 90; for 12 h;Inert atmosphere;
Steps:
142 Preparation of N-(3-(2-((2-fluoro-4-((1-methylpiperidin-4-yl)amino)phenyl)amino)quinazolin-8-yl)phenyl)acrylamide
To a solution of 4-bromo-2-fluoro-1-nitrobenzene (2.2 g, 10 mmol, 1 eq.) and 3- (4,4,5,5-tetramethyl-l,3,2-dioxaborolan-2-yl)aniline (3.81g, 15 mmol, 1.5 eq.) in dioxane (80 mL) was added KOAc (1.96 g, 20 mmol, 2 eq.), followed by Pd(dppf)Cl2(408 mg, 0.5 mmol, 0.05 eq.) under N2protection. The mixture was stirred at 90 °C for 12 h, then cooled to r.t. and concentrated. The resulting residue was purified via column chromatography(PE/EA=20/1~ 5/1, v/v) to afford 2-(3-fluoro-4-nitrophenyl)-4,4,5,5-tetramethyl-l,3,2- dioxaborolane as a white solid (2.1 g, 78.6% yield).
References:
Location in patent:Paragraph 0426
2369-13-3
246 suppliers
$19.00/5g
73183-34-3
556 suppliers
$6.00/5g
939968-60-2
40 suppliers
$71.00/100mg