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HuagongsheHuagongshe Chemie-Druckbericht · Nur für Forschungszwecke
HRID 80614Erstellt: 26. Oktober 2026

Water → (8S)-9-(2-chlorobenzyl)-2-(morpholin-4-yl)-8-(trifluoro-methyl)-6,7,8,9-tetrahydro-4H-pyrimido[1,2-a]pyrimidin-4-one

https://huagongshe.com/reaction/80614

Reaktionsgleichung

Beteiligte Stoffe

RolleNameHCIDEinwaage
EduktWaterHCID 962—
EduktCesium carbonateHCID 10796—
Eduktalpha-Bromo-o-chlorotolueneHCID 11905—
Edukt(S)-8-(Morpholin-4-yl)-2-(trifluoromethyl)-1,2,3,4-tetrahydropyrimido[1,2-a]pyrimidin-6-oneHCID 136238743—
LösungsmittelDimethylformamideHCID 6228—
Produkt(8S)-9-(2-chlorobenzyl)-2-(morpholin-4-yl)-8-(trifluoro-methyl)-6,7,8,9-tetrahydro-4H-pyrimido[1,2-a]pyrimidin-4-oneHCID 49854196—

Reaktionsschritte

214 mg of caesium carbonate and 74 mg of 1-(bromomethyl)-2-chlorobenzene are added to a solution of 100 mg of (8S)-2-(morpholin-4-yl)-8-(trifluoromethyl)-6,7,8,9-tetrahydro-4H-pyrimido[1,2-a]pyrimidin-4-one (Example 1e) in 2 ml of dimethylformamide. After 16 hours at a temperature in the region of 20° C., the reaction medium is run into water. The organic phase is separated and the aqueous phase is extracted with ethyl acetate. The combined organic phases are concentrated to dryness under reduced pressure. The residue is purified by preparative HPLC/MS (Method C). After evaporation of the acetonitrile and lyophilization, 94 mg of (8S)-9-(2-chloro-benzyl)-2-(morpholin-4-yl)-8-(trifluoromethyl)-6,7,8,9-tetrahydro-4H-pyrimido[1,2-a]pyrimidin-4-one are obtained in the form of an oil, the characteristics of which are the following:

Herkunft & Nachweise

DOI10.6084/m9.figshare.5104873.v1
PatentnummerUS08846670B2
Quelldatensatzuspto-grants-2014_09
ORD IDord-59858c38fb89486182308dde46b4b38f
Quellennotizuspto-grants-2014_09