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HRID 8484作成日:2026年10月23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/8484

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(3S)-3-Methyl-7,8-difluoro-2,3-dihydro-4H-1,4-benzoxazineHCID 11041424—
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 1108955788%

反応手順

To DMF (2.5 ml) was added potassium tertiary-butoxide (75 mg) under ice-cooling. After dropping a solution of the compound (100 mg) obtained in Example 78 and diethyl ethoxymethylenemalonate (233 mg) in DMF (0.5 ml), the resultant mixture was stirred for 2 hours. After treating in a conventional manner, the obtained residue was subjected to silica gel column chromatography to thereby give 153 mg (88%) of the title compound as an oily product. 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-4eb0b563d26541c38317838c6ee3f3f4
出典メモuspto-grants-2006_08