Zurück
HuagongsheHuagongshe Chemie-Druckbericht · Nur für Forschungszwecke
HRID 8475Erstellt: 24. Oktober 2026

Diethyl (ethoxymethylene)malonate → (S)-Diethyl (7,8-Difluoro-3-Methyl-3,4-Dihydro-2H-[1,4]Benzoxazin-4-Yl)Methylene-Malonate

https://huagongshe.com/de/reaction/8475

Reaktionsgleichung

Beteiligte Stoffe

RolleNameHCIDEinwaage
EduktDiethyl (ethoxymethylene)malonateHCID 6871—
Edukt(2S)-2-(2,3,4-Trifluoroanilino)propanolHCID 11401466—
EduktPotassium tert-butoxideHCID 23665647—
LösungsmittelDimethylformamideHCID 6228—
Produkt(S)-Diethyl (7,8-Difluoro-3-Methyl-3,4-Dihydro-2H-[1,4]Benzoxazin-4-Yl)Methylene-MalonateHCID 1108955765,2%

Reaktionsschritte

To DMF (2 ml) was added potassium tertiary-butoxide (226 mg) under ice-cooling. After dropping a solution of the compound (100 mg) obtained in Example 51 and diethyl ethoxymethylenemalonate (293 mg) in DMF (0.5 ml), the resultant mixture was stirred at room temperature for 18 hours. After treating in a conventional manner, the obtained residue was subjected to silica gel column chromatography to thereby give 113 mg (65%) of the title compound. The physical constants of the obtained compounds was identical with those described in Japanese Patent No. 2,769,174.

Herkunft & Nachweise

DOI10.6084/m9.figshare.5104873.v1
PatentnummerUS07087778B2
Quelldatensatzuspto-grants-2006_08
ORD IDord-03f445e855fe427bb8ab9a84c995bd04
Quellennotizuspto-grants-2006_08