5-cyclopropyl-2-fluoropyridine synthesis
- Product Name:5-cyclopropyl-2-fluoropyridine
- CAS Number:1034467-80-5
- Molecular formula:C8H8FN
- Molecular Weight:137.15
766-11-0
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Yield: 72%
Reaction Conditions:
with palladium diacetate;tricyclohexylphosphine in 1,2-dimethoxyethane;water at 80;
Steps:
16 5-cyclopropyl-2-fluoropyridine
A mixture of 5-bromo-2-fluoropyridine (435 mg, 2.5 mmol), cyclopropylboronic acid (260 mg, 3.0 mmol), potassium phosphate (1.27 g, 6.0 mmol), palladium (II) acetate (56 mg, 0.6 mmol) and tricyclohexyl phosphine (340 mg, 1.2 mmol) in 1,2- dimethoxyethane/water (10.0 mL/2.0 mL) was stirred at 80 °C overnight. The mixture was cooled and concentrated to dryness. The residue was purified by flash chromatography (petroleum ether / ethyl acetate = 3/1) to afford 5-cyclopropyl-2- fluoropyridine (246 mg, 1.8 mmol, 72% yield) as yellow solid. LCMS: m/z = 138.1 [M+H]+, retention time = 2.25 min (Method A).
References:
AKEBIA THERAPEUTICS, INC. WO2021/188944, 2021, A1 Location in patent:Paragraph 0432-0433
171197-80-1
292 suppliers
$20.00/1g
411235-57-9
435 suppliers
$6.00/1g
1034467-80-5
45 suppliers
$45.00/10mg