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ChemicalBook CAS DataBase List Imatinib

Imatinib synthesis

7synthesis methods
201230-82-2 Synthesis
carbon monoxide

201230-82-2
1 suppliers
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152460-10-1 Synthesis
N-(5-Amino-2-methylphenyl)-4-(3-pyridyl)-2-pyrimidineamine

152460-10-1
509 suppliers
$21.00/5g

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Yield:152459-95-5 95.8%

Reaction Conditions:

with palladium diacetate;triethylamine;4,5-bis(diphenylphosphino)-9,9-dimethylxanthene in 1,4-dioxane at 50; under 760.051 Torr; for 36 h;Inert atmosphere;Reagent/catalyst;Solvent;Temperature;

Steps:

1-4 Example 3

N-(5-amino-2-methylphenyl)-4-(pyridin-3-yl)pyrimidin-2-amine 0.1mol, 1-[(4-bromophenyl)methyl]-4-methyl 0.1mol of piperazine, 5mmol of palladium acetate, 5mmol of 4,5-bisdiphenylphosphine-9,9-dimethylxanthene and 0.18mol of triethylamine were added to 200mL of dioxane and replaced with nitrogen twice, Replace it with carbon monoxide twice, and heat to 50° C. under a carbon monoxide atmosphere (1 atm) with stirring for 36 hours. After the reaction is completed, the temperature is cooled down and replaced with nitrogen. The reaction solution is poured into 1L of water and filtered with suction. The obtained solid is recrystallized with methanol/dichloromethane (1/3, V/V). An off-white solid was obtained with a yield of 95.8%

References:

CN112125882,2020,A Location in patent:Paragraph 0033; 0041-0048

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