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HuagongsheHuagongshe Chemie-Druckbericht · Nur für Forschungszwecke
HRID 80610Erstellt: 24. Oktober 2026

Benzoyl chloride → (S)-9-benzoyl-2-morpholin-4-yl-8-trifluoromethyl-6,7,8,9-tetrahydropyrimido[1,2-a]pyrimidin-4-one

https://huagongshe.com/de/reaction/80610

Reaktionsgleichung

Beteiligte Stoffe

RolleNameHCIDEinwaage
EduktBenzoyl chlorideHCID 7412—
EduktSodium hydrideHCID 24758—
EduktSodium BicarbonateHCID 516892—
Edukt(S)-8-(Morpholin-4-yl)-2-(trifluoromethyl)-1,2,3,4-tetrahydropyrimido[1,2-a]pyrimidin-6-oneHCID 136238743—
LösungsmittelTetrahydrofuranHCID 8028—
LösungsmittelEthyl AcetateHCID 8857—
Produkt(S)-9-benzoyl-2-morpholin-4-yl-8-trifluoromethyl-6,7,8,9-tetrahydropyrimido[1,2-a]pyrimidin-4-oneHCID 49854090—

Reaktionsschritte

35.7 mg of sodium hydride and then, after 10 minutes of stirring, 0.135 ml de of benzoyl chloride are added, under an argon atmosphere, to a solution of 300 mg of (S)-2-morpholin-4-yl-8-trifluoromethyl-6,7,8,9-tetrahydropyrimido[1,2-a]pyrimidin-4-one (Example 1e) in 3 ml of tetrahydrofuran. After stirring for six hours at ambient temperature, a saturated solution of sodium bicarbonate and ethyl acetate are added to the reaction mixture. The organic phase is separated and then successively washed with a saturated solution of sodium chloride, dried over magnesium sulphate, filtered and concentrated under reduced pressure. The residue obtained is purified by silica chromatography (eluent: CH2Cl2) so as to give 74 mg of (S)-9-benzoyl-2-morpholin-4-yl-8-trifluoromethyl-6,7,8,9-tetrahydropyrimido[1,2-a]pyrimidin-4-one, in the form of a white solid, the characteristics of which are the following:

Herkunft & Nachweise

DOI10.6084/m9.figshare.5104873.v1
PatentnummerUS08846670B2
Quelldatensatzuspto-grants-2014_09
ORD IDord-66222c9585074824a8d726bdf81f9c07
Quellennotizuspto-grants-2014_09