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HuagongsheHuagongshe Chemie-Druckbericht · Nur für Forschungszwecke
HRID 520673Erstellt: 25. Oktober 2026

1-Ethyl-3-(3'-dimethylaminopropyl)carbodiimide → 4-(4-(1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamido)-2,5-difluorophenoxy)picolinamide

https://huagongshe.com/reaction/520673

Reaktionsgleichung

Beteiligte Stoffe

RolleNameHCIDEinwaage
Edukt1-Ethyl-3-(3'-dimethylaminopropyl)carbodiimideHCID 15908—
EduktHOAtHCID 181649—
EduktAntipyric acidHCID 246564—
Edukt4-(4-Amino-2,5-difluorophenoxy)pyridine-2-carboxamideHCID 24788628—
LösungsmittelDichloromethaneHCID 6344—
LösungsmittelEthyl AcetateHCID 8857—
Produkt4-(4-(1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamido)-2,5-difluorophenoxy)picolinamideHCID 7305092064%

Reaktionsbedingungen

Temperatur45 °C

Reaktionsschritte

To a solution of 4-(4-amino-2,5-difluorophenoxy)picolinamide (200 mg, 0.76 mmol), and 1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxylic acid (165 mg, 0.75 mmol) in DCM (10 mL) was added EDCI (175 mg, 0.93 mmol), and HOAT (26 mg, 0.15 mmol). The reaction was stirred at 45° C. for 16 hours, cooled to rt and diluted with EtOAc (20 mL). The solid was collected through filtration, dried at 45° C. in vacuo overnight to give the title compound as a white solid (230 mg, 63.7%).

Herkunft & Nachweise

DOI10.6084/m9.figshare.5104873.v1
PatentnummerUS09326975B2
Quelldatensatzuspto-grants-2016_05
ORD IDord-ab7d1b55eac745b5a5aaeb4dd9213999
Quellennotizuspto-grants-2016_05