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HRID 45999作成日:2026年10月27日

Triethylamine → 2-((1-Benzyl-4-(4-cyclopropylpiperazin-1-yl)-piperidin-4-yl)methyl)isoindolin-1-one

https://huagongshe.com/reaction/45999

反応式

関与物質

役割名称HCID仕込み量
反応物TriethylamineHCID 8471—
反応物Methyl 2-(bromomethyl)benzoateHCID 2734813—
反応物(1-Benzyl-4-(4-cyclopropylpiperazin-1-yl)piperidin-4-yl)methanamineHCID 57989589—
溶媒BenzeneHCID 241—
生成物2-((1-Benzyl-4-(4-cyclopropylpiperazin-1-yl)-piperidin-4-yl)methyl)isoindolin-1-oneHCID 5798959051%

反応手順

To a solution of (1-benzyl-4-(4-cyclopropylpiperazin-1-yl)piperidin-4-yl)methanamine (see above: synthesis of amine AM12) (1.22 mmol, 1.0 equiv.) and methyl 2-(bromomethyl)benzoate (1.22 mmol, 1.0 equiv.) in benzene (3 ml/mmol) was added triethylamine (2.44 mmol, 2.0 equiv.) and the resulting reaction mixture was refluxed for 25 h. The mixture was cooled to room temperature and the solvent was evaporated under reduced pressure. The residue was dissolved in ethyl acetate and the organic layer was successively washed with water and brine. The organic layer was dried over sodium sulfate and the solvent was evaporated under reduced pressure to give the crude product which was purified by silica gel column chromatography. Yield: 51%.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08541573B2
出典データセットuspto-grants-2013_09
ORD IDord-feca17fae52f41da8e02615f3d8018a8
出典メモuspto-grants-2013_09