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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 119Generated: October 28, 2026

1H-Pyrazole-1-carboxylicacid,3-amino-5-methyl-,1,1-dimethylethylester → 4-N-[1-(3,5-difluoro-2-pyridinyl)ethyl]-5-fluoro-2-N-(5-methyl-1H-pyrazol-3-yl)-6-morpholin-4-ylpyrimidine-2,4-diamine

https://huagongshe.com/reaction/119

Reaction equation

Participants

RoleNameHCIDCharge
Reactant1H-Pyrazole-1-carboxylicacid,3-amino-5-methyl-,1,1-dimethylethylesterHCID 11321537—
ReactantHCID 78133295HCID 78133295—
ReagentCesium carbonateHCID 10796—
Catalyst1,1'-(9,9-Dimethyl-9H-xanthene-4,5-diyl)bis(1,1-diphenylphosphine)HCID 636044—
CatalystBis(dibenzylideneacetone)palladiumHCID 9811564—
Solvent1,4-DioxaneHCID 31275—
Product4-N-[1-(3,5-difluoro-2-pyridinyl)ethyl]-5-fluoro-2-N-(5-methyl-1H-pyrazol-3-yl)-6-morpholin-4-ylpyrimidine-2,4-diamineHCID 251030380%

Reaction Conditions

Temperature110 °C

Reaction Steps

9,9-Dimethyl-4,5-bis(diphenylphosphino)xanthene (27.9 mg, 0.05 mmol), 2-chloro-N-(1-(3,5-difluoropyridin-2-yl)ethyl)-5-fluoro-6-morpholinopyrimidin-4-amine (200 mg, 0.54 mmol), tert-butyl 3-amino-5-methyl-1H-pyrazole-1-carboxylate (127 mg, 0.64 mmol) and cesium carbonate (349 mg, 1.07 mmol) were added to dioxane (8 mL). The mixture was purged with nitrogen for 15 minutes. Pd2(dba)3 (29.4 mg, 0.03 mmol) was added and the mixture heated at 110 °C for 3h. No sign of any reaction.

Provenance & Evidence

Source dataset750 AstraZeneca ELN dataset
ORD IDord-20af979b60da4f278f5b92ae2abaf8ca
Source note750 AstraZeneca ELN dataset