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HRID 1801986作成日:2026年10月25日

2-Ethylpropanedioyl dichloride → Ethyl 4-hydroxy-1-methyl-2-oxo-7-(trifluoromethyl)-1,2-dihydro-1,8-naphthyridine-3-carboxylate

https://huagongshe.com/reaction/1801986

反応式

関与物質

役割名称HCID仕込み量
反応物2-Ethylpropanedioyl dichlorideHCID 10920924—
反応物Methyl 2-(methylamino)-6-(trifluoromethyl)nicotinateHCID 57671595—
反応物Methyl 2-(3-ethoxy-N-methyl-3-oxopropanamido)-6-(trifluoromethyl)nicotinateHCID 57671654—
溶媒1,2-DichloroethaneHCID 11—
生成物Ethyl 4-hydroxy-1-methyl-2-oxo-7-(trifluoromethyl)-1,2-dihydro-1,8-naphthyridine-3-carboxylateHCID 57671568—

反応条件

温度80 °C

反応手順

Methyl 2-(3-ethoxy-N-methyl-3-oxopropanamido)-6-(trifluoromethyl)nicotinate. A mixture of methyl 2-(methylamino)-6-(trifluoromethyl)nicotinate (0.300 g) and ethyl malonoyl chloride (0.19 mL, 1.6 mmol) in 1,2-dichloroethane (50 mL) was heated to 80° C. for 63 hours. The reaction mixture was allowed to reach room temperature and was then evaporated under reduced pressure. The residue was purified by silica gel column chromatography (gradient: 0-30% EtOAc/hexanes) to give the title compound. MS (ESI, pos. ion) m/z: 349 (M+1).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08349868B2
出典データセットuspto-grants-2013_01
ORD IDord-6d147c0ed63041f3bbd432cdfb0da141
出典メモuspto-grants-2013_01