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HRID 337043作成日:2026年10月24日

Phenol → 4-Methyl-3-(2-oxo-3-phenoxy-1(2H)-pyrazinyl)-benzoic acid, methyl ester

https://huagongshe.com/ja/reaction/337043

反応式

関与物質

役割名称HCID仕込み量
反応物PhenolHCID 996—
反応物1,4-CyclohexadieneHCID 12343—
反応物DiisopropylethylamineHCID 81531—
反応物methyl 3-(3,5-dibromo-2-oxopyrazin-1(2H)-yl)-4-methylbenzoateHCID 66688740—
触媒PalladiumHCID 23938—
溶媒TetrahydrofuranHCID 8028—
生成物4-Methyl-3-(2-oxo-3-phenoxy-1(2H)-pyrazinyl)-benzoic acid, methyl esterHCID 86663239—

反応条件

温度120 °C

反応手順

A mixture of 3-(3,5-dibromo-2-oxo-2H-pyrazin-1-yl)-4-methyl-benzoic acid, methyl ester (Example 1b, 400 mg), phenol (400 mg), N,N-diisopropylethylamine (0.4 mL) and tetrahydrofuran (2 mL) was heated within a microwave for 3 h at 120° C. before being cooled to room temperature. The mixture was transferred to a mixture of palladium on carbon (10%, 38 mg) and tetrahydrofuran (1 mL). 1,4-Cyclohexadiene (2 mL) was added and the mixture was heated under atmosphere of nitrogen within a microwave for 15 minutes at 90° C. before being cooled to room temperature. The mixture was filtered and concentrated to give a crude product that was used in the next step without purification.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08889692B2
出典データセットuspto-grants-2014_11
ORD IDord-772973e7b197498ab8a77ab4301a1b29
出典メモuspto-grants-2014_11