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HRID 83607作成日:2026年10月23日

1,2-Dichloroethane → (1-(4-fluorobenzyl)-1H-indol-2-yl)(4-(piperidine-1-carbonyl)piperidin-1-yl)methanone

https://huagongshe.com/ja/reaction/83607

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DiisopropylethylamineHCID 81531—
反応物1-(Piperidin-4-ylcarbonyl)piperidineHCID 2794688—
反応物1-(4-fluorobenzyl)-1H-indole-2-carboxylic acidHCID 18627069—
溶媒DimethylformamideHCID 6228—
溶媒Diethylether ethylacetateHCID 21584169—
生成物(1-(4-fluorobenzyl)-1H-indol-2-yl)(4-(piperidine-1-carbonyl)piperidin-1-yl)methanoneHCID 6657109734.8%

反応手順

The following was added sequentially to anhydrous DMF (2 mL): 1-(4-fluorobenzyl)-1H-indole-2-carboxylic acid (50 mg, 0.186 mmol), Hunig's Base (0.065 ml, 0.371 mmol), EDC (46.3 mg, 0.241 mmol), HOBT (37.0 mg, 0.241 mmol), and piperidin-1-yl(piperidin-4-yl)methanone (36.4 mg, 0.186 mmol). The solution was allowed to stir at room temperature for 24 h. At this time, a 1:1 solution of diethylether/ethyl acetate (5 mL) was added, and this was washed with aqueous 10% Na2CO3 (3×2 mL). The extract was then dried with anhydrous MgSO4, filtered, and the filtrate was concentrated in vacuo. The crude residue was purified by column chromatography (20 g silica, 80% EtOAc/Hex) to provide 29 mg of the title compound.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08846684B2
出典データセットuspto-grants-2014_09
ORD IDord-7bc0b766889840ecb2fa528f206d1e58
出典メモuspto-grants-2014_09