4-Chloro-2-fluorophenylboronic acid synthesis
- Product Name:4-Chloro-2-fluorophenylboronic acid
- CAS Number:160591-91-3
- Molecular formula:C6H5BClFO2
- Molecular Weight:174.37
121-43-7
355 suppliers
$14.00/25mL
1996-29-8
316 suppliers
$6.00/5g
7732-18-5
471 suppliers
$13.50/100ML
160591-91-3
205 suppliers
$6.00/250mg
Yield:160591-91-3 81%
Reaction Conditions:
Stage #1: 1-bromo-4-chloro-2-fluorobenzenewith n-butyllithium in tetrahydrofuran;hexane at -78; for 1 h;
Stage #2: Trimethyl borate in tetrahydrofuran;hexane; for 0.5 h;
Stage #3: waterwith hydrogenchloride in tetrahydrofuran;hexane at 20;
Steps:
3.1 1) Preparation of compound 1
A 2 L round bottom flask was charged with 1-bromo-4-chloro-2-fluorobenzene(1-bromo-4-chloro-2-fluorobenzene, 50 g, 238.7 mmol)And anhydrous tetrahydrofuran 900 ml was added and the mixture was cooled to -78°C with stirring.N-butyl lithium (2.5 M hexane solution; 100 ml, 250 mmol)And the mixture was stirred for 1 hour.Trimethylborate (31.9 ml, 286 mmol) was slowly added thereto,After 30 minutes, 600 ml of a 1N hydrogen chloride aqueous solution was addedThe temperature was raised to room temperature while stirring.The organic layer was separated, dried over anhydrous magnesium sulfate, and filtered. The mixture was distilled under reduced pressure, concentrated, and extracted with chloroform and hexaneAnd recrystallized to obtain Compound 1 (33.7 g, 193.3 mmol) in a yield of 81%.
References:
KR101680413,2016,B1 Location in patent:Paragraph 0129-0132
5419-55-6
376 suppliers
$12.00/5g
1996-29-8
316 suppliers
$6.00/5g
160591-91-3
205 suppliers
$6.00/250mg
121-43-7
355 suppliers
$14.00/25mL
6797-79-1
188 suppliers
$9.00/5g
160591-91-3
205 suppliers
$6.00/250mg