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HRID 408836作成日:2026年10月26日

Methanol → 1-(4-Bromophenyl)-9-methyl-2-(2,3,4-trifluorophenoxy)-1,9-dihydro-6H-purin-6-one

https://huagongshe.com/reaction/408836

反応式

関与物質

役割名称HCID仕込み量
反応物MethanolHCID 887—
反応物2,3,4-TrifluorophenolHCID 123174—
反応物1-(4-Bromophenyl)-2-chloro-9-methyl-1,9-dihydro-6H-purin-6-oneHCID 57614152—
溶媒DichloromethaneHCID 6344—
生成物1-(4-Bromophenyl)-9-methyl-2-(2,3,4-trifluorophenoxy)-1,9-dihydro-6H-purin-6-oneHCID 24744032—

反応条件

温度140 °C

反応手順

1-(4-Bromophenyl)-2-chloro-9-methyl-1,9-dihydro-6H-purin-6-one (150 mg, 0.4417 mmol) and 2,3,4-trifluorophenol (130.8 mg, 0.8834 mmol) are added to a vial, and the sealed mixture is heated with stirring at 140° C. for 23 h. Silica gel column chromatography (MeOH:CH2Cl2=0.5:99.5) gives the title compound as a white solid. 1H NMR (400 MHz, CDCl3) 7.66 (3H, m), 7.24 (2H, m), 7.00 (2H, m), 3.58 (3H, s). MS (M+1): 451.08; RT=1.31 min. The IC50 determined as described in Example 6 is 100 nanomolar or less.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08759361B2
出典データセットuspto-grants-2014_06
ORD IDord-dd9828272f7349498ffe3bde326c78ab
出典メモuspto-grants-2014_06