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HRID 983062作成日:2026年10月26日

1,2-Dichloroethane → 1-[4-(5,6,7,8-Tetrahydro-1H-pyrrolo[3,2-b]azepine-4-carbonyl)piperidin-1-yl]-ethanone

https://huagongshe.com/reaction/983062

反応式

関与物質

役割名称HCID仕込み量
反応物1,2-DichloroethaneHCID 11—
反応物1-HydroxybenzotriazoleHCID 75771—
反応物1-Acetylpiperidine-4-carboxylic acidHCID 117255—
反応物1,4,5,6,7,8-Hexahydropyrrolo[3,2-B]azepineHCID 22561790—
溶媒DichloromethaneHCID 6344—
生成物1-[4-(5,6,7,8-Tetrahydro-1H-pyrrolo[3,2-b]azepine-4-carbonyl)piperidin-1-yl]-ethanoneHCID 2256185895%

反応手順

To a mixture of 1-acetyl-piperidine-4-carboxylic acid (822 mg, 4.8 mmol, 1.2 eq.), EDC (920 mg, 1.2 eq.), HOBt (648 mg, 1.2 eq.) in DCM (15 mL) was added TEA (1.3 mL, 2 eq.) and 1,4,5,6,7,8-hexahydro-pyrrolo[3,2-b]azepine (550 mg, 4 mmol). The mixture was stirred at rt for 2 days. The reaction was diluted with DCM, washed with water, sat. NaHCO3, brine, dried and concentrated. The residue was purified on a silica gel column to give 1.1 g of 1-[4-(5,6,7,8-tetrahydro-1H-pyrrolo[3,2-b]azepine-4-carbonyl)-piperidin-1-yl]-ethanone as a white solid.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US06861418B2
出典データセットuspto-grants-2005_03
ORD IDord-6632b5eaed124fabb2dbfa3e4ac8df1b
出典メモuspto-grants-2005_03