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HRID 884596作成日:2026年10月26日

4-Bromobutyryl chloride → 5-{6-[(4-Bromo-butyrylamino)-methyl]-pyrimidin-4-yloxy}-indole-1-carboxylic acid (4-fluoro-3-trifluoromethyl-phenyl)-amide

https://huagongshe.com/reaction/884596

反応式

関与物質

役割名称HCID仕込み量
反応物4-Bromobutyryl chlorideHCID 70225—
反応物DiisopropylethylamineHCID 81531—
反応物5-(6-Aminomethyl-pyrimidin-4-yloxy)-indole-1-carboxylic acid (4-fluoro-3-trifluoromethyl-phenyl)-amideHCID 59394236—
溶媒DichloromethaneHCID 6344—
溶媒Ethyl AcetateHCID 8857—
生成物5-{6-[(4-Bromo-butyrylamino)-methyl]-pyrimidin-4-yloxy}-indole-1-carboxylic acid (4-fluoro-3-trifluoromethyl-phenyl)-amideHCID 59394487—

反応手順

5-(6-Aminomethyl-pyrimidin-4-yloxy)-indole-1-carboxylic acid (4-fluoro-3-trifluoromethyl-phenyl)-amide (52.5 mg, 0.117 mmol) is dissolved in DCM (5 mL) at 0° C. DIEA (0.025 mL, 0.143 mmol) is added followed by 4-bromo-butyryl chloride (0.020 mL, 0.172 mmol). The reaction is stirred for 30 min before being diluted with ethyl acetate and washed with water. The organic layer is removed, dried, and concentrated to provide the title compound. MS (ESI) m/z 595.6 (M+1).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08242125B2
出典データセットuspto-grants-2012_08
ORD IDord-2590b25cb7974e77af4d61930d5d801f
出典メモuspto-grants-2012_08