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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 472202Generated: October 29, 2026

Potassium Carbonate → 6-(5-(Aminomethyl)-2-fluorophenyl)-8-cyclopentyl-4-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one

https://huagongshe.com/reaction/472202

Reaction equation

Participants

RoleNameHCIDCharge
ReactantPotassium CarbonateHCID 11430—
Reactant1-(3-Bromo-4-fluorophenyl)methanamine hydrochlorideHCID 2724901—
Reactant8-Cyclopentyl-4-methyl-2-(methylamino)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-6-ylboronic acidHCID 59258886—
CatalystTetrakis(triphenylphosphine)palladiumHCID 11979704—
SolventEthanolHCID 702—
Solvent1,2-DimethoxyethaneHCID 8071—
Product6-(5-(Aminomethyl)-2-fluorophenyl)-8-cyclopentyl-4-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-oneHCID 5925900543.4%

Reaction Conditions

Temperature100 °C

Reaction Steps

To a solution of 8-cyclopentyl-4-methyl-2-(methylamino)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-6-ylboronic acid (30 mg, 0.099 mmol), 3-bromo-4-fluorobenzylamine hydrochloride (28.7 mg, 0.119 mmol), potassium carbonate (3 M, 0.10 mL) in DME (0.5 mL) and EtOH (0.5 mL) was added tetrakis(triphenylphosphine) palladium(0) (6 mg, 0.005 mmol). The mixture was degassed with N2, sealed and heated for 1 h at 100° C. in microwave. The mixture was removed under reduced pressure. The crude product was purified by chromatography to give the title compound (16.4 mg, 43.3%).

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS08633204B2
Source datasetuspto-grants-2014_01
ORD IDord-1ef461d01d094e719eb56fa9a5c5abb8
Source noteuspto-grants-2014_01