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HuagongsheHuagongshe Chemie-Druckbericht · Nur für Forschungszwecke
HRID 520439Erstellt: 23. Oktober 2026

Picolinic acid → N-(3-methyl-4-oxo-2-(3-(trifluoromethyl)phenyl)-3,4-dihydroquinazolin-8-yl)picolinamide

https://huagongshe.com/de/reaction/520439

Reaktionsgleichung

Beteiligte Stoffe

RolleNameHCIDEinwaage
EduktPicolinic acidHCID 1018—
EduktDiisopropylethylamineHCID 81531—
EduktMethanaminium, N-((dimethylamino)(3H-1,2,3-triazolo(4,5-b)pyridin-3-yloxy)methylene)-N-methyl-, hexafluorophosphate(1-) (1:1)HCID 9886157—
Edukt8-amino-3-methyl-2-(3-(trifluoromethyl)phenyl)quinazolin-4(3H)-oneHCID 58552822—
LösungsmittelWaterHCID 962—
LösungsmittelDiethyl EtherHCID 3283—
LösungsmittelDimethylformamideHCID 6228—
ProduktN-(3-methyl-4-oxo-2-(3-(trifluoromethyl)phenyl)-3,4-dihydroquinazolin-8-yl)picolinamideHCID 4525514993%

Reaktionsbedingungen

Temperatur55 °C

Reaktionsschritte

A mixture of 8-amino-3-methyl-2-(3-(trifluoromethyl)phenyl)quinazolin-4(3H)-one 5 (106 mg, 0.33 mmol), pyridine-2-carboxylic acid 6 (84 mg, 0.68 mmol), HATU (263 mg, 0.69 mmo) and DIPEA (208 mg) in DMF were heated at 55° C. for 2.5 h then poured into H2O. The resulting precipitate was collected by filtration, rinsed with H2O, then Et2O to give Compound 239 as a yellow solid (130 mg, 93% yield). MS (ESI) calc. for C22H15F3N4O2: 424.11. found: 425 [M+H].

Herkunft & Nachweise

DOI10.6084/m9.figshare.5104873.v1
PatentnummerUS09326986B2
Quelldatensatzuspto-grants-2016_05
ORD IDord-50d484079dd847f5b3902c0eeb4e7211
Quellennotizuspto-grants-2016_05