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HuagongsheHuagongshe Chemie-Druckbericht · Nur für Forschungszwecke
HRID 556626Erstellt: 26. Oktober 2026

Ethylenediamine → 2-[(2-Aminoethyl)amino]-8-(2,6-difluorophenyl)-4-(4-fluoro-2-methylphenyl)pyrido[2,3-d]pyrimidin-7(8H)-one

https://huagongshe.com/reaction/556626

Reaktionsgleichung

Beteiligte Stoffe

RolleNameHCIDEinwaage
EduktEthylenediamineHCID 3301—
Edukt8-(2,6-difluoro-phenyl)-4-(4-fluoro-2-methyl-phenyl)-2-methanesulfonyl-8H-pyrido[2,3-d]pyrimidin-7-oneHCID 59639554—
LösungsmittelTetrahydrofuranHCID 8028—
LösungsmittelWater ethylacetateHCID 22728543—
Produkt2-[(2-Aminoethyl)amino]-8-(2,6-difluorophenyl)-4-(4-fluoro-2-methylphenyl)pyrido[2,3-d]pyrimidin-7(8H)-oneHCID 5963957789,6%

Reaktionsschritte

The title compound of Example 48 [8-(2,6-difluorophenyl)-4-(4-fluoro-2-methylphenyl)-2-methanesulfonyl-8H-pyrido[2,3-d]pyrimidin-7-one] (0.89 g, 0.002 mol) in dry THF, stirring at 23°, under Ar, was treated with ethylenediamine (668 uL, 0.01 mol). The color became orange. LC MS showed no starting material after 5 min. Reaction was stripped to dryness; the residue taken up in EtOAc-H2O. The layers were separated and the aq phase adjusted to pH 10.5 with 10% NaOH. Aq phase was extracted twice with EtOAc; combined organic layers were dried (Na2SO4), then evaporated to give 0.762 g (89%) of the title compound as a glass. LC MS (m/e)=426 (MH+). Rt=1.52 min.

Herkunft & Nachweise

DOI10.6084/m9.figshare.5104873.v1
PatentnummerUS08058282B2
Quelldatensatzuspto-grants-2011_11
ORD IDord-ded6eac52ee7406f80938e7010fa718c
Quellennotizuspto-grants-2011_11