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HRID 400500作成日:2026年10月27日

Sodium Carbonate → N-(2,6-difluorophenyl)-3-[(8aS)-hexahydropyrrolo[1,2-a]pyrazin-2(1H)-ylcarbonyl]benzenesulfonamide

https://huagongshe.com/reaction/400500

反応式

関与物質

役割名称HCID仕込み量
反応物Sodium CarbonateHCID 10340—
反応物Benzoyl chloride, 3-(chlorosulfonyl)-HCID 77671—
反応物2,6-DifluoroanilineHCID 79647—
反応物(6S)-1,4-Diazabicyclo(4.3.0)nonaneHCID 781249—
溶媒DichloromethaneHCID 6344—
生成物N-(2,6-difluorophenyl)-3-[(8aS)-hexahydropyrrolo[1,2-a]pyrazin-2(1H)-ylcarbonyl]benzenesulfonamideHCID 46853383—

反応手順

To 3-(chlorosulfonyl)benzoyl chloride (0.474 g, 1.98 mmol) in anhydrous dichloromethane (10 mL) was added (S)-octahydropyrrolo[1,2-a]pyrazine (0.250 g, 1.98 mmol) in dichloromethane (4 mL) slowly over 10 minutes at room temperature. Then sodium carbonate (0.420 g, 3.96 mmol) was added. The mixture was stirred at room temperature for 5 hours. Then 2,6-difluoroaniline (2.56 g, 19.81 mmol) was added. The mixture was stirred at room temperature overnight and then concentrated. The residue was purified by chromatography on silica gel (dichloromethane, then methanol/dichloromethane=1:10) to give the title compound.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08741899B2
出典データセットuspto-grants-2014_06
ORD IDord-7ba525e0068c4cafb6c8ebee64517b7d
出典メモuspto-grants-2014_06