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HRID 1873839作成日:2026年10月26日

Diisopropylethylamine → 1-[2-(Methylsulfonyl)-4-(trifluoromethoxy)benzoyl]-4-(1-methyl-1-{[3-(trifluoromethyl)phenyl]sulfonyl}ethyl)piperidine

https://huagongshe.com/reaction/1873839

反応式

関与物質

役割名称HCID仕込み量
反応物DiisopropylethylamineHCID 81531—
反応物Benzotriazol-1-yloxy-tris(dimethylamino)phosphonium hexafluorophosphateHCID 151348—
反応物HCID 59447309HCID 59447309—
反応物4-(1-Methyl-1-{[3-(trifluoromethyl)phenyl]sulfonyl}ethyl)piperidineHCID 59447409—
溶媒Dimethyl SulfoxideHCID 679—
溶媒WaterHCID 962—
溶媒DimethylformamideHCID 6228—
溶媒Trifluoroacetic acidHCID 6422—
生成物1-[2-(Methylsulfonyl)-4-(trifluoromethoxy)benzoyl]-4-(1-methyl-1-{[3-(trifluoromethyl)phenyl]sulfonyl}ethyl)piperidineHCID 25255784—

反応手順

To a 10 ml vial was added 4-(1-methyl-1-{[3-(trifluoromethyl)phenyl]sulfonyl}ethyl)piperidine (70.8 mg, 0.211 mmol), 2-(methylsulfonyl)-4-(trifluoromethoxy)benzoic acid (50 mg, 0.176 mmol), Bop reagent (93 mg, 0.211 mmol), diisopropylethyl amine (0.062 ml, 0.352 mmol) and 2 ml dimethylformamide. The resulting solution was stirred at room temperature for 10 minutes. The reaction mixture was diluted with 1 ml dimethyl sulfoxide, 1 ml water and 0.03 ml of trifluoroacetic acid. This mixture was loaded on a reverse phase column and purified with HPLC eluted with water/acetonitrile gradient solvent. Desired fraction was collected and lyophilized to give to give title compound as fluffy white solid.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08304434B2
出典データセットuspto-grants-2012_11
ORD IDord-66f474659cc04294a5f14145823fbc0c
出典メモuspto-grants-2012_11