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HRID 45859作成日:2026年10月24日

4-(Trifluoromethyl)phenyl isocyanate → 1-(3-{4-[2-(tert-butylamino)pyridin-4-yl]-1-(4-methoxybenzyl)-1H-pyrazol-3-yl}phenyl)-3-[4-(trifluoromethyl)phenyl]urea

https://huagongshe.com/ja/reaction/45859

反応式

関与物質

役割名称HCID仕込み量
反応物4-(Trifluoromethyl)phenyl isocyanateHCID 73768—
反応物SodiumHCID 5360545—
反応物4-[3-(3-aminophenyl)-1-(4-methoxybenzyl)-1H-pyrazol-4-yl]-N-tert-butyl-pyridin-2-amineHCID 67184018—
溶媒DimethylformamideHCID 6228—
生成物1-(3-{4-[2-(tert-butylamino)pyridin-4-yl]-1-(4-methoxybenzyl)-1H-pyrazol-3-yl}phenyl)-3-[4-(trifluoromethyl)phenyl]ureaHCID 6718478560%

反応手順

350 mg (0.82 mmol) of 4-[3-(3-aminophenyl)-1-(4-methoxybenzyl)-1H-pyrazol-4-yl]-N-tert-butyl-pyridin-2-amine were dissolved in 30 ml of dry dimethylformamide and 110 μl (0.82 mmol) of p-trifluoromethyl-phenyl isocyanate were added to the resulting solution. The mixture was stirred overnight at room temperature, then poured into an aqueous solution of sodium hydrogenocarbonate and extracted with dichloromethane. The organic phase was dried over sodium sulphate and evaporated in vacuo. The residue was chromatographed on a silica gel column (dichloromethane-acetone 9/1), affording 302 mg (60%) of the title compound.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08541575B2
出典データセットuspto-grants-2013_09
ORD IDord-1e25fcda39bd496e89515e1abb5c512d
出典メモuspto-grants-2013_09