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HRID 28513作成日:2026年10月24日

Sodium Carbonate → 3-[2(R)-{ethoxycarbonylpropyl-amino}-2-phenylethyl]-5-(2-chloro-3-methoxyphenyl)-1-[2-fluoro-6-(trifluoromethyl)benzyl]pyrimidine-2,4(1H,3H)-dione

https://huagongshe.com/ja/reaction/28513

反応式

関与物質

役割名称HCID仕込み量
反応物Sodium CarbonateHCID 10340—
反応物Ethyl 4-bromobutyrateHCID 76300—
反応物(R)-1-(2-fluoro-6-(trifluoromethyl)benzyl)-3-(2-amino-2-phenylethyl)-5-(2-chloro-3-methoxyphenyl)pyrimidine-2,4(1H,3H)-dioneHCID 11376252—
溶媒DimethylformamideHCID 6228—
生成物3-[2(R)-{ethoxycarbonylpropyl-amino}-2-phenylethyl]-5-(2-chloro-3-methoxyphenyl)-1-[2-fluoro-6-(trifluoromethyl)benzyl]pyrimidine-2,4(1H,3H)-dioneHCID 8659651053.4%

反応条件

温度95 °C

反応手順

To a solution of compound 7h (2.0 g, 3.65 mmol) in DMF (8 mL) was added Na2CO3 (0.47 g, 4.38 mmol) followed by ethyl 4-bromobutyrate (0.83 mL, 5.48 mmol). The mixture was heated at 95° C. for 1.5 hours, cooled to room temperature, and partitioned between ethyl acetate and H2O. The organic layer was washed with brine, dried over Na2SO4 and concentrated. The residue was purified by column chromatography on silica gel with ethyl acetate/hexanes/triethylamine 500/500/5 to afford compound 7i (1.29 g) as a white solid. MS (CI) m/z 662.2, 664.2 (MH+)

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07419983B2
出典データセットuspto-grants-2008_09
ORD IDord-d0fc61949e4c4ac1b1d8d452feff5a9a
出典メモuspto-grants-2008_09