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HRID 8475作成日:2026年10月24日

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

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

反応式

関与物質

役割名称HCID仕込み量
反応物Diethyl (ethoxymethylene)malonateHCID 6871—
反応物(2S)-2-(2,3,4-Trifluoroanilino)propanolHCID 11401466—
反応物Potassium tert-butoxideHCID 23665647—
溶媒DimethylformamideHCID 6228—
生成物(S)-Diethyl (7,8-Difluoro-3-Methyl-3,4-Dihydro-2H-[1,4]Benzoxazin-4-Yl)Methylene-MalonateHCID 1108955765.2%

反応手順

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.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07087778B2
出典データセットuspto-grants-2006_08
ORD IDord-03f445e855fe427bb8ab9a84c995bd04
出典メモuspto-grants-2006_08