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HRID 68469作成日:2026年10月24日

Triethylamine → 5-Chloro-N-{[(5S)-3-(3-isopropyl-2-oxo-2,3-dihydro-1,3-benzoxazol-6-yl)-2-oxo-1,3-oxazolidin-5-yl]methyl}-2-thiophenecarboxamide

https://huagongshe.com/ja/reaction/68469

反応式

関与物質

役割名称HCID仕込み量
反応物TriethylamineHCID 8471—
反応物5-Chlorothiophene-2-carbonyl ChlorideHCID 589223—
反応物6-[(5S)-5-(aminomethyl)-2-oxo-1,3-oxazolidin-3-yl]-3-isopropyl-1,3-benzoxazol-2(3H)-one hydrochlorideHCID 57496662—
溶媒TetrahydrofuranHCID 8028—
生成物5-Chloro-N-{[(5S)-3-(3-isopropyl-2-oxo-2,3-dihydro-1,3-benzoxazol-6-yl)-2-oxo-1,3-oxazolidin-5-yl]methyl}-2-thiophenecarboxamideHCID 57496661—

反応手順

200 mg (0.61 mmol) of 6-[(5S)-5-(aminomethyl)-2-oxo-1,3-oxazolidin-3-yl]-3-isopropyl-1,3-benzoxazol-2(3H)-one hydrochloride (EP 738726) are suspended in 5 ml of tetrahydrofuran and admixed with 0.26 ml (1.83 mmol) of triethylamine and 132 mg (0.73 mmol) of 5-chlorothiophene-2-carbonyl chloride. The reaction mixture is stirred at room temperature overnight and then concentrated. The product is isolated by column chromatography (silica gel, methylene chloride/ethanol=50/1 to 20/1). This gives 115 mg (43% of theory) of the desired compound.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08822458B2
出典データセットuspto-grants-2014_09
ORD IDord-40ac4258f5644bfdaf57abffed19acfc
出典メモuspto-grants-2014_09