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HRID 130681作成日:2026年10月25日

Water → Tradipitant

https://huagongshe.com/reaction/130681

反応式

関与物質

役割名称HCID仕込み量
反応物WaterHCID 962—
反応物Potassium CarbonateHCID 11430—
反応物1-(Azidomethyl)-3,5-bis(trifluoromethyl)benzeneHCID 44185743—
反応物(2-Chlorophenyl)-[2-(2-hydroxy-2-pyridin-4-yl-vinyl)pyridin-3-yl]methanoneHCID 136347867—
溶媒IsopropanolHCID 3776—
生成物TradipitantHCID 9916461—

反応条件

温度20 °C

反応手順

The reaction can also be carried out using (2-chlorophenyl)-[2-(2-hydroxy-2-pyridin-4-yl-vinyl)pyridin-3-yl]methanone (30.0 g; 72.3 mmol; 1.0 equiv) in isopropanol (225 mL). 1-azidomethyl-3,5-bistrifluoromethylbenzene (20.43 g; 76 mmol; 1.05 equiv) and potassium carbonate (5.0 g; 36.2 mmol; 0.5 equiv) are added, and the reaction mixture is heated to reflux for 21-24 hours. Cool the reaction mixture to 20° C., add water (120 mL), and stir for approximately 16 hours. Filter, wash with 120 mL isopropanol/water (1:1 v/v), and dry under reduced pressure at 50° C. to yield the title compound, which may be recrystallized as described above.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07381826B2
出典データセットuspto-grants-2008_06
ORD IDord-4783d67d115340ea998b33d74f29b382
出典メモuspto-grants-2008_06