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HRID 45134作成日:2026年10月24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/ja/reaction/45134

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US08541432B2
出典データセットuspto-grants-2013_09
ORD IDord-957f92fc0b514c5a9ed5ca74bdf74659
出典メモuspto-grants-2013_09