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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 533Generated: October 28, 2026

HCID 169489376, compound → 4-[[(2S,4R)-1-(5-chloro-1-methylpyrazole-4-carbonyl)-2-methylpiperidin-4-yl]amino]-6,7-difluoro-1H-quinolin-2-one

https://huagongshe.com/reaction/533

Reaction equation

Participants

RoleNameHCIDCharge
ReactantHCID 169489376HCID 169489376—
ReactantHCID 178418196HCID 178418196—
ReagentCesium carbonateHCID 10796—
CatalystBinap, (A+-)-HCID 634876—
CatalystPalladium (II) acetateHCID 4144353—
SolventTolueneHCID 1140—
Product4-[[(2S,4R)-1-(5-chloro-1-methylpyrazole-4-carbonyl)-2-methylpiperidin-4-yl]amino]-6,7-difluoro-1H-quinolin-2-oneHCID 9068248449.46%

Reaction Conditions

Temperature140 °C

Reaction Steps

4-chloro-6,7-difluoroquinolin-2(1H)-one (100 mg, 0.46 mmol) was taken in a microwave tube. Added ((2S,4R)-4-amino-2-methylpiperidin-1-yl)(5-chloro-1-methyl-1H-pyrazol-4-yl)methanone 2,2,2-trifluoroacetate (172 mg, 0.46 mmol), followed by the addition of Palladium (II) acetate (10.41 mg, 0.05 mmol), racemic-2,2'-Bis(diphenylphosphino)-1,1'-binaphthyl (28.9 mg, 0.05 mmol), Cesium carbonate (111 mL, 1.39 mmol), N,N'-Diisopropylethylamine (242 mL, 1.39 mmol). toluene (10 mL) was added and subjected to microwave with the following parameters. Temperature 140 °C Time 60 minutes After the completion of the reaction, dissolved the compound in methanol and purified by column

Provenance & Evidence

Source dataset750 AstraZeneca ELN dataset
ORD IDord-d1c1c91e4e404216818f2894a49b5c96
Source note750 AstraZeneca ELN dataset